Charles S. Craik, PhD

Pharmaceutical Chemistry
+1 415 476-8146

My research interests focus on defining the roles and the mechanisms of enzymes and other challenging proteins in complex biological processes and on developing technologies to facilitate these studies. The current research in the Craik lab focuses on the chemical biology of proteolytic and protein degradation enzymes, receptors and membrane transporters. A particular emphasis of our work is on identifying the roles and regulating the activity of key proteins associated with infectious diseases, neurodegeneration and cancer. I am also interested in developing novel methods to biophysically characterize challenging proteins as well as their complexes. These studies coupled with our global substrate profiling, antibody engineering and noninvasive imaging efforts are providing a better understanding of both the chemical make-up and the biological importance of these critical proteins to aid in the rapid detection, monitoring and control of infectious disease, neurological disorders and cancer. This in turn is leading to the development of strategies for regulating these activities as a means of therapeutic intervention. Further study of these proteins holds promise for better understanding, rapid detection and eventual control of infectious diseases, cancer and neurodegeneration.


Structural basis of prostaglandin efflux by MRP4.

Nature structural & molecular biology

Pourmal S, Green E, Bajaj R, Chemmama IE, Knudsen GM, Gupta M, Sali A, Cheng Y, Craik CS, Kroetz DL, Stroud RM

Preparing for the next pandemic.

Science (New York, N.Y.)

Shoichet BK, Craik CS

Proteases influence colony aggregation behavior in Vibrio cholerae.

The Journal of biological chemistry

Detomasi TC, Batka AE, Valastyan JS, Hydorn MA, Craik CS, Bassler BL, Marletta MA

Rare antibody phage isolation and discrimination (RAPID) biopanning enables identification of high-affinity antibodies against challenging targets.

Communications biology

Chung DH, Kong S, Young NJ, Chuo SW, Shiah JV, Connelly EJ, Rohweder PJ, Born A, Manglik A, Grandis JR, Johnson DE, Craik CS

Phosphorylation of a Cleaved Tau Proteoform at a Single Residue Inhibits Binding to the E3 Ubiquitin Ligase, CHIP.

bioRxiv : the preprint server for biology

Nadel CM, Wucherer K, Oehler A, Thwin AC, Basu K, Callahan MD, Southworth DR, Mordes DA, Craik CS, Gestwicki JE

Large library docking for novel SARS-CoV-2 main protease non-covalent and covalent inhibitors.

Protein science : a publication of the Protein Society

Fink EA, Bardine C, Gahbauer S, Singh I, Detomasi T, White K, Gu S, Wan X, Chen J, Ary B, Glenn I, O'Connell J, O'Donnell H, Fajtová P, Lyu J, Vigneron S, Young NJ, Kondratov IS, Alisoltani A, Simons LM, Lorenzo-Redondo R, Ozer EA, Hultquist JF, O'Donoghue AJ, Moroz Y, Taunton J, Renslo AR, Irwin JJ, García-Sastre A, Shoichet BK, Craik CS

A Prototype Assay Multiplexing SARS-CoV-2 3CL-Protease and Angiotensin-Converting Enzyme 2 for Saliva-Based Diagnostics in COVID-19.


Suresh V, Sheik DA, Detomasi TC, Zhao T, Zepeda T, Saladi S, Rajesh UC, Byers K, Craik CS, Davisson VJ

The E3 Ubiquitin Ligase, CHIP/STUB1, Inhibits Aggregation of Phosphorylated Proteoforms of Microtubule-associated Protein Tau (MAPT).

Journal of molecular biology

Nadel CM, Thwin AC, Callahan M, Lee K, Connelly E, Craik CS, Southworth DR, Gestwicki JE

Correction: Mutations in α-synuclein, TDP-43 and tau prolong protein half-life through diminished degradation by lysosomal proteases.

Molecular neurodegeneration

Sampognaro PJ, Arya S, Knudsen GM, Gunderson EL, Sandoval-Perez A, Hodul M, Bowles K, Craik CS, Jacobson MP, Kao AW

Discovery and Characterization of Antibody Probes of Module 2 of the 6-Deoxyerythronolide B Synthase.


Guzman KM, Cogan DP, Brodsky KL, Soohoo AM, Li X, Sevillano N, Mathews II, Nguyen KP, Craik CS, Khosla C

Perturbations in podocyte transcriptome and biological pathways induced by FSGS associated circulating factors.

Annals of translational medicine

Rashmi P, Sigdel TK, Rychkov D, Damm I, Da Silva AA, Vincenti F, Lourenco AL, Craik CS, Reiser J, Sarwal MM

Mutations in a-synuclein, TDP-43 and tau prolong protein half-life through diminished degradation by lysosomal proteases.

Molecular neurodegeneration

Sampognaro PJ, Arya S, Knudsen GM, Gunderson EL, Sandoval-Perez A, Hodul M, Bowles K, Craik CS, Jacobson MP, Kao AW

High-throughput optofluidic screening of single B cells identifies novel cross-reactive antibodies as inhibitors of uPAR with antibody-dependent effector functions.


Louren?o AL, Chuo SW, Bohn MF, Hann B, Khan S, Yevalekar N, Patel N, Yang T, Xu L, Lv D, Drakas R, Lively S, Craik CS

Multiplex substrate profiling by mass spectrometry for proteases.

Methods in enzymology

Rohweder PJ, Jiang Z, Hurysz BM, O'Donoghue AJ, Craik CS

Accurate Identification of Mucinous Pancreatic Cystic Lesions Using Small-Volume Analytes.

The Journal of surgical research

Caiazza F, Conroy PC, Ivry SL, York T, Lin J, Hernandez S, Hoffmann TJ, Francis SS, Park WG, Yip-Schneider MT, Schmidt CM, Brand R, Craik CS, Kirkwood K

Incidence and prevalence of COVID-19 within a healthcare worker cohort during the first year of the SARS-CoV-2 pandemic.

Clinical infectious diseases : an official publication of the Infectious Diseases Society of America

Doernberg SB, Holubar M, Jain V, Weng Y, Lu D, Bollyky JB, Sample H, Huang B, Craik CS, Desai M, Rutherford GW, Maldonado Y, CHART Study Consortium

A covalent inhibitor of K-Ras(G12C) induces MHC class I presentation of haptenated peptide neoepitopes targetable by immunotherapy.

Cancer cell

Zhang Z, Rohweder PJ, Ongpipattanakul C, Basu K, Bohn MF, Dugan EJ, Steri V, Hann B, Shokat KM, Craik CS

Structure-function analysis of enterovirus protease 2A in complex with its essential host factor SETD3.

Nature communications

Peters CE, Schulze-Gahmen U, Eckhardt M, Jang GM, Xu J, Pulido EH, Bardine C, Craik CS, Ott M, Gozani O, Verba KA, Hüttenhain R, Carette JE, Krogan NJ

Structure-Based Identification of Naphthoquinones and Derivatives as Novel Inhibitors of Main Protease Mpro and Papain-like Protease PLpro of SARS-CoV-2.

Journal of chemical information and modeling

Santos LH, Kronenberger T, Almeida RG, Silva EB, Rocha REO, Oliveira JC, Barreto LV, Skinner D, Fajtová P, Giardini MA, Woodworth B, Bardine C, Lourenço AL, Craik CS, Poso A, Podust LM, McKerrow JH, Siqueira-Neto JL, O'Donoghue AJ, da Silva Júnior EN, Ferreira RS

Translation of a Protease Turnover Assay for Clinical Discrimination of Mucinous Pancreatic Cysts.

Diagnostics (Basel, Switzerland)

Suresh V, Byers K, Rajesh UC, Caiazza F, Zhu G, Craik CS, Kirkwood K, Davisson VJ, Sheik DA

Inhibiting a dynamic viral protease by targeting a non-catalytic cysteine.

Cell chemical biology

Hulce KR, Jaishankar P, Lee GM, Bohn MF, Connelly EJ, Wucherer K, Ongpipattanakul C, Volk RF, Chuo SW, Arkin MR, Renslo AR, Craik CS

Structure-based identification of naphthoquinones and derivatives as novel inhibitors of main protease Mpro and papain-like protease PLpro of SARS-CoV-2.

bioRxiv : the preprint server for biology

Santos LH, Kronenberger T, Almeida RG, Silva EB, Rocha REO, Oliveira JC, Barreto LV, Skinner D, Fajtová P, Giardini MA, Woodworth B, Bardine C, Lourenço AL, Craik CS, Poso A, Podust LM, McKerrow JH, Siqueira-Neto JL, O'Donoghue AJ, da Silva Júnior EN, Ferreira RS

Colloidal Aggregators in Biochemical SARS-CoV-2 Repurposing Screens.

Journal of medicinal chemistry

O'Donnell HR, Tummino TA, Bardine C, Craik CS, Shoichet BK

Design of a population-based longitudinal cohort study of SARS-CoV-2 incidence and prevalence among adults in the San Francisco Bay Area.

Annals of epidemiology

Lindan CP, Desai M, Boothroyd D, Judson T, Bollyky J, Sample H, Weng Y, Cheng Y, Dahlen A, Hedlin H, Grumbach K, Henne J, Garcia S, Gonzales R, Craik CS, Maldonado Y, Rutherford G

Mapping the catalytic conformations of an assembly-line polyketide synthase module.

Science (New York, N.Y.)

Cogan DP, Zhang K, Li X, Li S, Pintilie GD, Roh SH, Craik CS, Chiu W, Khosla C

A novel class of TMPRSS2 inhibitors potently block SARS-CoV-2 and MERS-CoV viral entry and protect human epithelial lung cells.

Proceedings of the National Academy of Sciences of the United States of America

Mahoney M, Damalanka VC, Tartell MA, Chung DH, Lourenço AL, Pwee D, Mayer Bridwell AE, Hoffmann M, Voss J, Karmakar P, Azouz NP, Klingler AM, Rothlauf PW, Thompson CE, Lee M, Klampfer L, Stallings CL, Rothenberg ME, Pöhlmann S, Whelan SPJ, O'Donoghue AJ, Craik CS, Janetka JW

Immunotargeting of Nanocrystals by SpyCatcher Conjugation of Engineered Antibodies.

ACS nano

Pedroso CCS, Mann VR, Zuberbühler K, Bohn MF, Yu J, Altoe V, Craik CS, Cohen BE

Characterising proteolysis during SARS-CoV-2 infection identifies viral cleavage sites and cellular targets with therapeutic potential.

Nature communications

Meyer B, Chiaravalli J, Gellenoncourt S, Brownridge P, Bryne DP, Daly LA, Grauslys A, Walter M, Agou F, Chakrabarti LA, Craik CS, Eyers CE, Eyers PA, Gambin Y, Jones AR, Sierecki E, Verdin E, Vignuzzi M, Emmott E

In Vivo Measurement of Granzyme Proteolysis from Activated Immune Cells with PET.

ACS central science

Zhao N, Bardine C, Lourenço AL, Wang YH, Huang Y, Cleary SJ, Wilson DM, Oh DY, Fong L, Looney MR, Evans MJ, Craik CS

Colloidal aggregators in biochemical SARS-CoV-2 repurposing screens.

bioRxiv : the preprint server for biology

Oâ Donnell HR, Tummino TA, Bardine C, Craik CS, Shoichet BK

Re-emerging Aspartic Protease Targets: Examining Cryptococcus neoformans Major Aspartyl Peptidase 1 as a Target for Antifungal Drug Discovery.

Journal of medicinal chemistry

Kryštufek R, Šácha P, Starková J, Brynda J, Hradilek M, Tloušt'ová E, Grzymska J, Rut W, Boucher MJ, Drag M, Majer P, Hájek M, Rezácová P, Madhani HD, Craik CS, Konvalinka J

Identification of recombinant Fabs for structural and functional characterization of HIV-host factor complexes.

PloS one

Sevillano N, Green EM, Votteler J, Kim DY, Ren X, Yang B, Liu X, Lourenço AL, Hurley JH, Farr-Jones S, Gross JD, Cheng Y, Craik CS

A novel class of TMPRSS2 inhibitors potently block SARS-CoV-2 and MERS-CoV viral entry and protect human epithelial lung cells.

bioRxiv : the preprint server for biology

Mahoney M, Damalanka VC, Tartell MA, Chung DH, Lourenco AL, Pwee D, Mayer Bridwell AE, Hoffmann M, Voss J, Karmakar P, Azouz N, Klingler AM, Rothlauf PW, Thompson CE, Lee M, Klampfer L, Stallings C, Rothenberg ME, Pöhlmann S, Whelan SP, O'Donoghue AJ, Craik CS, Janetka JW

Structural insight into SARS-CoV-2 neutralizing antibodies and modulation of syncytia.


Asarnow D, Wang B, Lee WH, Hu Y, Huang CW, Faust B, Ng PML, Ngoh EZX, Bohn M, Bulkley D, Pizzorno A, Ary B, Tan HC, Lee CY, Minhat RA, Terrier O, Soh MK, Teo FJ, Yeap YYC, Seah SGK, Chan CEZ, Connelly E, Young NJ, Maurer-Stroh S, Renia L, Hanson BJ, Rosa-Calatrava M, Manglik A, Cheng Y, Craik CS, Wang CI

Global Protease Activity Profiling Identifies HER2-Driven Proteolysis in Breast Cancer.

ACS chemical biology

Salcedo EC, Winter MB, Khuri N, Knudsen GM, Sali A, Craik CS

Platform to Discover Protease-Activated Antibiotics and Application to Siderophore-Antibiotic Conjugates.

Journal of the American Chemical Society

Boyce JH, Dang B, Ary B, Edmondson Q, Craik CS, DeGrado WF, Seiple IB

Structural and mechanistic basis of the EMC-dependent biogenesis of distinct transmembrane clients.


Miller-Vedam LE, Bräuning B, Popova KD, Schirle Oakdale NT, Bonnar JL, Prabu JR, Boydston EA, Sevillano N, Shurtleff MJ, Stroud RM, Craik CS, Schulman BA, Frost A, Weissman JS

Structure of an affinity-matured inhibitory recombinant fab against urokinase plasminogen activator reveals basis of potency and specificity.

Biochimica et biophysica acta. Proteins and proteomics

Sevillano N, Bohn MF, Zimanyi M, Chen Y, Petzold C, Gupta S, Ralston CY, Craik CS

An Analysis of Isoclonal Antibody Formats Suggests a Role for Measuring PD-L1 with Low Molecular Weight PET Radiotracers.

Molecular imaging and biology

Wei J, Wang YH, Lee CY, Truillet C, Oh DY, Xu Y, Ruggero D, Flavell RR, VanBrocklin HF, Seo Y, Craik CS, Fong L, Wang CI, Evans MJ

Antibody Probes of Module 1 of the 6-Deoxyerythronolide B Synthase Reveal an Extended Conformation During Ketoreduction.

Journal of the American Chemical Society

Cogan DP, Li X, Sevillano N, Mathews II, Matsui T, Craik CS, Khosla C

Bivalent binding of a fully human IgG to the SARS-CoV-2 spike proteins reveals mechanisms of potent neutralization.

bioRxiv : the preprint server for biology

Wang B, Asarnow D, Lee WH, Huang CW, Faust B, Ng PML, Ngoh EZX, Bohn M, Bulkley D, Pizzorno A, Tan HC, Lee CY, Minhat RA, Terrier O, Soh MK, Teo FJ, Yeap YYC, Hu Y, Seah SGK, Maurer-Stroh S, Renia L, Hanson BJ, Rosa-Calatrava M, Manglik A, Cheng Y, Craik CS, Wang CI

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.


Gordon DE, Jang GM, Bouhaddou M, Xu J, Obernier K, White KM, O'Meara MJ, Rezelj VV, Guo JZ, Swaney DL, Tummino TA, Huettenhain R, Kaake RM, Richards AL, Tutuncuoglu B, Foussard H, Batra J, Haas K, Modak M, Kim M, Haas P, Polacco BJ, Braberg H, Fabius JM, Eckhardt M, Soucheray M, Bennett MJ, Cakir M, McGregor MJ, Li Q, Meyer B, Roesch F, Vallet T, Mac Kain A, Miorin L, Moreno E, Naing ZZC, Zhou Y, Peng S, Shi Y, Zhang Z, Shen W, Kirby IT, Melnyk JE, Chorba JS, Lou K, Dai SA, Barrio-Hernandez I, Memon D, Hernandez-Armenta C, Lyu J, Mathy CJP, Perica T, Pilla KB, Ganesan SJ, Saltzberg DJ, Rakesh R, Liu X, Rosenthal SB, Calviello L, Venkataramanan S, Liboy-Lugo J, Lin Y, Huang XP, Liu Y, Wankowicz SA, Bohn M, Safari M, Ugur FS, Koh C, Savar NS, Tran QD, Shengjuler D, Fletcher SJ, O'Neal MC, Cai Y, Chang JCJ, Broadhurst DJ, Klippsten S, Sharp PP, Wenzell NA, Kuzuoglu D, Wang HY, Trenker R, Young JM, Cavero DA, Hiatt J, Roth TL, Rathore U, Subramanian A, Noack J, Hubert M, Stroud RM, Frankel AD, Rosenberg OS, Verba KA, Agard DA, Ott M, Emerman M, Jura N, von Zastrow M, Verdin E, Ashworth A, Schwartz O, d'Enfert C, Mukherjee S, Jacobson M, Malik HS, Fujimori DG, Ideker T, Craik CS, Floor SN, Fraser JS, Gross JD, Sali A, Roth BL, Ruggero D, Taunton J, Kortemme T, Beltrao P, Vignuzzi M, García-Sastre A, Shokat KM, Shoichet BK, Krogan NJ

Monitoring protease activity in biological tissues using antibody prodrugs as sensing probes.

Scientific reports

Vasiljeva O, Menendez E, Nguyen M, Craik CS, Michael Kavanaugh W

A SARS-CoV-2-Human Protein-Protein Interaction Map Reveals Drug Targets and Potential Drug-Repurposing.

bioRxiv : the preprint server for biology

Gordon DE, Jang GM, Bouhaddou M, Xu J, Obernier K, O'Meara MJ, Guo JZ, Swaney DL, Tummino TA, Hüttenhain R, Kaake RM, Richards AL, Tutuncuoglu B, Foussard H, Batra J, Haas K, Modak M, Kim M, Haas P, Polacco BJ, Braberg H, Fabius JM, Eckhardt M, Soucheray M, Bennett MJ, Cakir M, McGregor MJ, Li Q, Naing ZZC, Zhou Y, Peng S, Kirby IT, Melnyk JE, Chorba JS, Lou K, Dai SA, Shen W, Shi Y, Zhang Z, Barrio-Hernandez I, Memon D, Hernandez-Armenta C, Mathy CJP, Perica T, Pilla KB, Ganesan SJ, Saltzberg DJ, Ramachandran R, Liu X, Rosenthal SB, Calviello L, Venkataramanan S, Lin Y, Wankowicz SA, Bohn M, Trenker R, Young JM, Cavero D, Hiatt J, Roth T, Rathore U, Subramanian A, Noack J, Hubert M, Roesch F, Vallet T, Meyer B, White KM, Miorin L, Agard D, Emerman M, Ruggero D, García-Sastre A, Jura N, von Zastrow M, Taunton J, Schwartz O, Vignuzzi M, d'Enfert C, Mukherjee S, Jacobson M, Malik HS, Fujimori DG, Ideker T, Craik CS, Floor S, Fraser JS, Gross J, Sali A, Kortemme T, Beltrao P, Shokat K, Shoichet BK, Krogan NJ

Isoforms of Cathepsin B1 in Neurotropic Schistosomula of Trichobilharzia regenti Differ in Substrate Preferences and a Highly Expressed Catalytically Inactive Paralog Binds Cystatin.

Frontiers in cellular and infection microbiology

Dvoráková H, Leontovyc R, Machácek T, O'Donoghue AJ, Šedo O, Zdráhal Z, Craik CS, Caffrey CR, Horák P, Mikeš L

Further Evidence that the Soluble Urokinase Plasminogen Activator Receptor Does Not Directly Injure Mice or Human Podocytes.


Harel E, Shoji J, Abraham V, Miller L, Laszik ZG, King A, Dobi D, Szabo G, Hann B, Sarwal MM, Craik CS, Vincenti F

The lysosomal aminopeptidase tripeptidyl peptidase 1 displays increased activity in malignant pancreatic cysts.

Biological chemistry

Ivry SL, Knudsen GM, Caiazza F, Sharib JM, Jaradeh K, Ravalin M, O'Donoghue AJ, Kirkwood KS, Craik CS

End-Binding E3 Ubiquitin Ligases Enable Protease Signaling.

ACS chemical biology

Ravalin M, Basu K, Gestwicki JE, Craik CS

Antibody-Drug Conjugates Targeting the Urokinase Receptor (uPAR) as a Possible Treatment of Aggressive Breast Cancer.

Antibodies (Basel, Switzerland)

Harel ET, Drake PM, Barfield RM, Lui I, Farr-Jones S, Van't Veer L, Gartner ZJ, Green EM, Lourenço AL, Cheng Y, Hann BC, Rabuka D, Craik CS

KH-Type Splicing Regulatory Protein Controls Colorectal Cancer Cell Growth and Modulates the Tumor Microenvironment.

The American journal of pathology

Caiazza F, Oficjalska K, Tosetto M, Phelan JJ, Noonan S, Martin P, Killick K, Breen L, O'Neill F, Nolan B, Furney S, Power R, Fennelly D, Craik CS, O'Sullivan J, Sheahan K, Doherty GA, Ryan EJ

Specificity for latent C termini links the E3 ubiquitin ligase CHIP to caspases.

Nature chemical biology

Ravalin M, Theofilas P, Basu K, Opoku-Nsiah KA, Assimon VA, Medina-Cleghorn D, Chen YF, Bohn MF, Arkin M, Grinberg LT, Craik CS, Gestwicki JE

Why recombinant antibodies - benefits and applications.

Current opinion in biotechnology

Basu K, Green EM, Cheng Y, Craik CS

Identifying a potential biomarker for primary focal segmental glomerulosclerosis and its association with recurrence after transplantation.

Clinical transplantation

Harel E, Shoji J, Abraham V, Miller L, Laszik Z, Thurison T, King A, Olshen A, Leung J, Szabo G, Hann B, Høyer-Hansen G, Craik CS, Vincenti F

Progranulin Stimulates the in vitro Maturation of pro-Cathepsin D at Acidic pH.

Journal of molecular biology

Butler VJ, Cortopassi WA, Argouarch AR, Ivry SL, Craik CS, Jacobson MP, Kao AW

Discovery of Selective Matriptase and Hepsin Serine Protease Inhibitors: Useful Chemical Tools for Cancer Cell Biology.

Journal of medicinal chemistry

Damalanka VC, Han Z, Karmakar P, O'Donoghue AJ, La Greca F, Kim T, Pant S, Helander J, Klefström J, Craik CS, Janetka JW

Predicting CD4 T-cell epitopes based on antigen cleavage, MHCII presentation, and TCR recognition.

PloS one

Schneidman-Duhovny D, Khuri N, Dong GQ, Winter MB, Shifrut E, Friedman N, Craik CS, Pratt KP, Paz P, Aswad F, Sali A

Discovery and characterization of a thioesterase-specific monoclonal antibody that recognizes the 6-deoxyerythronolide B synthase.


Li X, Sevillano N, La Greca F, Hsu J, Mathews II, Matsui T, Craik CS, Khosla C

A preclinical assessment of 89Zr-atezolizumab identifies a requirement for carrier added formulations not observed with 89Zr-C4.

Bioconjugate chemistry

Moroz A, Lee CY, Wang YH, Hsiao JC, Sevillano N, Truillet C, Craik CS, Fong L, Wang CI, Evans MJ

Structural determinants of specificity and regulation of activity in the allosteric loop network of human KLK8/neuropsin.

Scientific reports

Debela M, Magdolen V, Skala W, Elsässer B, Schneider EL, Craik CS, Biniossek ML, Schilling O, Bode W, Brandstetter H, Goettig P

Structure-Function Analysis of the Extended Conformation of a Polyketide Synthase Module.

Journal of the American Chemical Society

Li X, Sevillano N, La Greca F, Deis L, Liu YC, Deller MC, Mathews II, Matsui T, Cane DE, Craik CS, Khosla C

SmSP2: A serine protease secreted by the blood fluke pathogen Schistosoma mansoni with anti-hemostatic properties.

PLoS neglected tropical diseases

Leontovyc A, Ulrychová L, O'Donoghue AJ, Vondrášek J, Marešová L, Hubálek M, Fajtová P, Chanová M, Jiang Z, Craik CS, Caffrey CR, Mareš M, Dvorák J, Horn M

Substrate Specificity of Cysteine Proteases Beyond the S2 Pocket: Mutagenesis and Molecular Dynamics Investigation of Fasciola hepatica Cathepsins L.

Frontiers in molecular biosciences

Corvo I, Ferraro F, Merlino A, Zuberbühler K, O'Donoghue AJ, Pastro L, Pi-Denis N, Basika T, Roche L, McKerrow JH, Craik CS, Caffrey CR, Tort JF

Fab-based inhibitors reveal ubiquitin independent functions for HIV Vif neutralization of APOBEC3 restriction factors.

PLoS pathogens

Binning JM, Smith AM, Hultquist JF, Craik CS, Caretta Cartozo N, Campbell MG, Burton L, La Greca F, McGregor MJ, Ta HM, Bartholomeeusen K, Peterlin BM, Krogan NJ, Sevillano N, Cheng Y, Gross JD

Cryo-EM structures of the TMEM16A calcium-activated chloride channel.


Dang S, Feng S, Tien J, Peters CJ, Bulkley D, Lolicato M, Zhao J, Zuberbühler K, Ye W, Qi L, Chen T, Craik CS, Jan YN, Minor DL, Cheng Y, Jan LY

Global substrate specificity profiling of post-translational modifying enzymes.

Protein science : a publication of the Protein Society

Ivry SL, Meyer NO, Winter MB, Bohn MF, Knudsen GM, O'Donoghue AJ, Craik CS

Immunoproteasome functions explained by divergence in cleavage specificity and regulation.


Winter MB, La Greca F, Arastu-Kapur S, Caiazza F, Cimermancic P, Buchholz TJ, Anderl JL, Ravalin M, Bohn MF, Sali A, O'Donoghue AJ, Craik CS

Imaging PD-L1 Expression with ImmunoPET.

Bioconjugate chemistry

Truillet C, Oh HLJ, Yeo SP, Lee CY, Huynh LT, Wei J, Parker MFL, Blakely C, Sevillano N, Wang YH, Shen YS, Olivas V, Jami KM, Moroz A, Jego B, Jaumain E, Fong L, Craik CS, Chang AJ, Bivona TG, Wang CI, Evans MJ

Biochemical Basis for Distinct Roles of the Heterochromatin Proteins Swi6 and Chp2.

Journal of molecular biology

Isaac RS, Sanulli S, Tibble R, Hornsby M, Ravalin M, Craik CS, Gross JD, Narlikar GJ

Allosteric Inhibitors, Crystallography, and Comparative Analysis Reveal Network of Coordinated Movement across Human Herpesvirus Proteases.

Journal of the American Chemical Society

Acker TM, Gable JE, Bohn MF, Jaishankar P, Thompson MC, Fraser JS, Renslo AR, Craik CS

Matriptase Induction of Metalloproteinase-Dependent Aggrecanolysis In Vitro and In Vivo: Promotion of Osteoarthritic Cartilage Damage by Multiple Mechanisms.

Arthritis & rheumatology (Hoboken, N.J.)

Wilkinson DJ, Habgood A, Lamb HK, Thompson P, Hawkins AR, Désilets A, Leduc R, Steinmetzer T, Hammami M, Lee MS, Craik CS, Watson S, Lin H, Milner JM, Rowan AD

Substrate Profiling and High Resolution Co-complex Crystal Structure of a Secreted C11 Protease Conserved across Commensal Bacteria.

ACS chemical biology

Roncase EJ, Moon C, Chatterjee S, González-Páez GE, Craik CS, O'Donoghue AJ, Wolan DW

Global Protease Activity Profiling Provides Differential Diagnosis of Pancreatic Cysts.

Clinical cancer research : an official journal of the American Association for Cancer Research

Ivry SL, Sharib JM, Dominguez DA, Roy N, Hatcher SE, Yip-Schneider MT, Schmidt CM, Brand RE, Park WG, Hebrok M, Kim GE, O'Donoghue AJ, Kirkwood KS, Craik CS

Synthesis and mechanistic evaluation of novel N'-benzylidene-carbohydrazide-1H-pyrazolo[3,4-b]pyridine derivatives as non-anionic antiplatelet agents.

European journal of medicinal chemistry

Lourenço AL, Salvador RRS, Silva LA, Saito MS, Mello JFR, Cabral LM, Rodrigues CR, Vera MAF, Muri EMF, de Souza AMT, Craik CS, Dias LRS, Castro HC, Sathler PC

Multiplex Substrate Profiling by Mass Spectrometry for Kinases as a Method for Revealing Quantitative Substrate Motifs.

Analytical chemistry

Meyer NO, O'Donoghue AJ, Schulze-Gahmen U, Ravalin M, Moss SM, Winter MB, Knudsen GM, Craik CS

Discovery of Reactive Microbiota-Derived Metabolites that Inhibit Host Proteases.


Guo CJ, Chang FY, Wyche TP, Backus KM, Acker TM, Funabashi M, Taketani M, Donia MS, Nayfach S, Pollard KS, Craik CS, Cravatt BF, Clardy J, Voigt CA, Fischbach MA

Integrated Activity and Genetic Profiling of Secreted Peptidases in Cryptococcus neoformans Reveals an Aspartyl Peptidase Required for Low pH Survival and Virulence.

PLoS pathogens

Clarke SC, Dumesic PA, Homer CM, O'Donoghue AJ, La Greca F, Pallova L, Majer P, Madhani HD, Craik CS

Clustering of disulfide-rich peptides provides scaffolds for hit discovery by phage display: application to interleukin-23.

BMC bioinformatics

Barkan DT, Cheng XL, Celino H, Tran TT, Bhandari A, Craik CS, Sali A, Smythe ML

Global Identification of Biofilm-Specific Proteolysis in Candida albicans.


Winter MB, Salcedo EC, Lohse MB, Hartooni N, Gulati M, Sanchez H, Takagi J, Hube B, Andes DR, Johnson AD, Craik CS, Nobile CJ

Procathepsin E is highly abundant but minimally active in pancreatic ductal adenocarcinoma tumors.

Biological chemistry

O'Donoghue AJ, Ivry SL, Chaudhury C, Hostetter DR, Hanahan D, Craik CS

Cysteine and Aspartyl Proteases Contribute to Protein Digestion in the Gut of Freshwater Planaria.

PLoS neglected tropical diseases

Goupil LS, Ivry SL, Hsieh I, Suzuki BM, Craik CS, O'Donoghue AJ, McKerrow JH

Label-Free Electrical Detection of Enzymatic Reactions in Nanochannels.

ACS nano

Duan C, Alibakhshi MA, Kim DK, Brown CM, Craik CS, Majumdar A

Design of Selective Substrates and Activity-Based Probes for Hydrolase Important for Pathogenesis 1 (HIP1) from Mycobacterium tuberculosis.

ACS infectious diseases

Lentz CS, Ordonez AA, Kasperkiewicz P, La Greca F, O'Donoghue AJ, Schulze CJ, Powers JC, Craik CS, Drag M, Jain SK, Bogyo M

Intracellular Action of a Secreted Peptide Required for Fungal Virulence.

Cell host & microbe

Homer CM, Summers DK, Goranov AI, Clarke SC, Wiesner DL, Diedrich JK, Moresco JJ, Toffaletti D, Upadhya R, Caradonna I, Petnic S, Pessino V, Cuomo CA, Lodge JK, Perfect J, Yates JR, Nielsen K, Craik CS, Madhani HD

Matriptase activation connects tissue factor-dependent coagulation initiation to epithelial proteolysis and signaling.


Le Gall SM, Szabo R, Lee M, Kirchhofer D, Craik CS, Bugge TH, Camerer E

Site-Specific Radiofluorination of Biomolecules with 8-[(18)F]-Fluorooctanoic Acid Catalyzed by Lipoic Acid Ligase.

ACS chemical biology

Drake CR, Sevillano N, Truillet C, Craik CS, VanBrocklin HF, Evans MJ

Quantitative MS-based enzymology of caspases reveals distinct protein substrate specificities, hierarchies, and cellular roles.

Proceedings of the National Academy of Sciences of the United States of America

Julien O, Zhuang M, Wiita AP, O'Donoghue AJ, Knudsen GM, Craik CS, Wells JA

Structure- and function-based design of Plasmodium-selective proteasome inhibitors.


Li H, O'Donoghue AJ, van der Linden WA, Xie SC, Yoo E, Foe IT, Tilley L, Craik CS, da Fonseca PC, Bogyo M

Fragment-Based Protein-Protein Interaction Antagonists of a Viral Dimeric Protease.


Gable JE, Lee GM, Acker TM, Hulce KR, Gonzalez ER, Schweigler P, Melkko S, Farady CJ, Craik CS

Complementary Proteomic and Biochemical Analysis of Peptidases in Lobster Gastric Juice Uncovers the Functional Role of Individual Enzymes in Food Digestion.

Marine biotechnology (New York, N.Y.)

Bibo-Verdugo B, O'Donoghue AJ, Rojo-Arreola L, Craik CS, García-Carreño F

In vivo imaging of protease activity by Probody therapeutic activation.


Wong KR, Menendez E, Craik CS, Kavanaugh WM, Vasiljeva O

Non-invasive imaging and cellular tracking of pulmonary emboli by near-infrared fluorescence and positron-emission tomography.

Nature communications

Page MJ, Lourenço AL, David T, LeBeau AM, Cattaruzza F, Castro HC, VanBrocklin HF, Coughlin SR, Craik CS

Excretion/secretion products from Schistosoma mansoni adults, eggs and schistosomula have unique peptidase specificity profiles.


Dvorák J, Fajtová P, Ulrychová L, Leontovyc A, Rojo-Arreola L, Suzuki BM, Horn M, Mareš M, Craik CS, Caffrey CR, O'Donoghue AJ

Destructin-1 is a collagen-degrading endopeptidase secreted by Pseudogymnoascus destructans, the causative agent of white-nose syndrome.

Proceedings of the National Academy of Sciences of the United States of America

O'Donoghue AJ, Knudsen GM, Beekman C, Perry JA, Johnson AD, DeRisi JL, Craik CS, Bennett RJ

Ecotin: Exploring a feasible antithrombotic profile.

International journal of biological macromolecules

Wermelinger LS, Frattani FS, Carneiro-Lobo TC, Craik CS, Castro HC, Zingali RB

Imaging active urokinase plasminogen activator in prostate cancer.

Cancer research

LeBeau AM, Sevillano N, Markham K, Winter MB, Murphy ST, Hostetter DR, West J, Lowman H, Craik CS, VanBrocklin HF

Structural requirements for the collagenase and elastase activity of cathepsin K and its selective inhibition by an exosite inhibitor.

The Biochemical journal

Sharma V, Panwar P, O'Donoghue AJ, Cui H, Guido RV, Craik CS, Brömme D

Subnanometre-resolution electron cryomicroscopy structure of a heterodimeric ABC exporter.


Kim J, Wu S, Tomasiak TM, Mergel C, Winter MB, Stiller SB, Robles-Colmanares Y, Stroud RM, Tampé R, Craik CS, Cheng Y

Structure-function analyses of human kallikrein-related peptidase 2 establish the 99-loop as master regulator of activity.

The Journal of biological chemistry

Skala W, Utzschneider DT, Magdolen V, Debela M, Guo S, Craik CS, Brandstetter H, Goettig P

Cullin E3 ligases and their rewiring by viral factors.


Mahon C, Krogan NJ, Craik CS, Pick E

The androgen-regulated protease TMPRSS2 activates a proteolytic cascade involving components of the tumor microenvironment and promotes prostate cancer metastasis.

Cancer discovery

Lucas JM, Heinlein C, Kim T, Hernandez SA, Malik MS, True LD, Morrissey C, Corey E, Montgomery B, Mostaghel E, Clegg N, Coleman I, Brown CM, Schneider EL, Craik C, Simon JA, Bedalov A, Nelson PS

Broad-spectrum allosteric inhibition of herpesvirus proteases.


Gable JE, Lee GM, Jaishankar P, Hearn BR, Waddling CA, Renslo AR, Craik CS

Urokinase-type plasminogen activator receptor (uPAR) ligation induces a raft-localized integrin signaling switch that mediates the hypermotile phenotype of fibrotic fibroblasts.

The Journal of biological chemistry

Grove LM, Southern BD, Jin TH, White KE, Paruchuri S, Harel E, Wei Y, Rahaman SO, Gladson CL, Ding Q, Craik CS, Chapman HA, Olman MA

Imaging the urokinase plasminongen activator receptor in preclinical breast cancer models of acquired drug resistance.


LeBeau AM, Sevillano N, King ML, Duriseti S, Murphy ST, Craik CS, Murphy LL, VanBrocklin HF

MEK-dependent negative feedback underlies BCR-ABL-mediated oncogene addiction.

Cancer discovery

Asmussen J, Lasater EA, Tajon C, Oses-Prieto J, Jun YW, Taylor BS, Burlingame A, Craik CS, Shah NP

Elastin degradation by cathepsin V requires two exosites.

The Journal of biological chemistry

Du X, Chen NL, Wong A, Craik CS, Brömme D

Global substrate profiling of proteases in human neutrophil extracellular traps reveals consensus motif predominantly contributed by elastase.

PloS one

O'Donoghue AJ, Jin Y, Knudsen GM, Perera NC, Jenne DE, Murphy JE, Craik CS, Hermiston TW

Dissecting the active site of the collagenolytic cathepsin L3 protease of the invasive stage of Fasciola hepatica.

PLoS neglected tropical diseases

Corvo I, O'Donoghue AJ, Pastro L, Pi-Denis N, Eroy-Reveles A, Roche L, McKerrow JH, Dalton JP, Craik CS, Caffrey CR, Tort JF

Substrate specificity of MarP, a periplasmic protease required for resistance to acid and oxidative stress in Mycobacterium tuberculosis.

The Journal of biological chemistry

Small JL, O'Donoghue AJ, Boritsch EC, Tsodikov OV, Knudsen GM, Vandal O, Craik CS, Ehrt S

Mutational tail loss is an evolutionary mechanism for liberating marapsins and other type I serine proteases from transmembrane anchors.

The Journal of biological chemistry

Raman K, Trivedi NN, Raymond WW, Ganesan R, Kirchhofer D, Verghese GM, Craik CS, Schneider EL, Nimishakavi S, Caughey GH

Targeting uPAR with antagonistic recombinant human antibodies in aggressive breast cancer.

Cancer research

LeBeau AM, Duriseti S, Murphy ST, Pepin F, Hann B, Gray JW, VanBrocklin HF, Craik CS

Imaging a functional tumorigenic biomarker in the transformed epithelium.

Proceedings of the National Academy of Sciences of the United States of America

LeBeau AM, Lee M, Murphy ST, Hann BC, Warren RS, Delos Santos R, Kurhanewicz J, Hanash SM, VanBrocklin HF, Craik CS

Mapping inhibitor binding modes on an active cysteine protease via nuclear magnetic resonance spectroscopy.


Lee GM, Balouch E, Goetz DH, Lazic A, McKerrow JH, Craik CS

Global identification of peptidase specificity by multiplex substrate profiling.

Nature methods

O'Donoghue AJ, Eroy-Reveles AA, Knudsen GM, Ingram J, Zhou M, Statnekov JB, Greninger AL, Hostetter DR, Qu G, Maltby DA, Anderson MO, Derisi JL, McKerrow JH, Burlingame AL, Craik CS

Activity and inhibition of prostasin and matriptase on apical and basolateral surfaces of human airway epithelial cells.

American journal of physiology. Lung cellular and molecular physiology

Nimishakavi S, Besprozvannaya M, Raymond WW, Craik CS, Gruenert DC, Caughey GH

Characterization of gut-associated cathepsin D hemoglobinase from tick Ixodes ricinus (IrCD1).

The Journal of biological chemistry

Sojka D, Franta Z, Frantová H, Bartosová P, Horn M, Váchová J, O'Donoghue AJ, Eroy-Reveles AA, Craik CS, Knudsen GM, Caffrey CR, McKerrow JH, Mares M, Kopácek P

Fabs enable single particle cryoEM studies of small proteins.

Structure (London, England : 1993)

Wu S, Avila-Sakar A, Kim J, Booth DS, Greenberg CH, Rossi A, Liao M, Li X, Alian A, Griner SL, Juge N, Yu Y, Mergel CM, Chaparro-Riggers J, Strop P, Tampé R, Edwards RH, Stroud RM, Craik CS, Cheng Y

Investigation of the proteolytic functions of an expanded cercarial elastase gene family in Schistosoma mansoni.

PLoS neglected tropical diseases

Ingram JR, Rafi SB, Eroy-Reveles AA, Ray M, Lambeth L, Hsieh I, Ruelas D, Lim KC, Sakanari J, Craik CS, Jacobson MP, McKerrow JH

Analysis of Fasciola cathepsin L5 by S2 subsite substitutions and determination of the P1-P4 specificity reveals an unusual preference.


Norbury LJ, Hung A, Beckham S, Pike RN, Spithill TW, Craik CS, Choe Y, Fecondo JV, Smooker PM

Global landscape of HIV-human protein complexes.


Jäger S, Cimermancic P, Gulbahce N, Johnson JR, McGovern KE, Clarke SC, Shales M, Mercenne G, Pache L, Li K, Hernandez H, Jang GM, Roth SL, Akiva E, Marlett J, Stephens M, D'Orso I, Fernandes J, Fahey M, Mahon C, O'Donoghue AJ, Todorovic A, Morris JH, Maltby DA, Alber T, Cagney G, Bushman FD, Young JA, Chanda SK, Sundquist WI, Kortemme T, Hernandez RD, Craik CS, Burlingame A, Sali A, Frankel AD, Krogan NJ

Vif hijacks CBF-ß to degrade APOBEC3G and promote HIV-1 infection.


Jäger S, Kim DY, Hultquist JF, Shindo K, LaRue RS, Kwon E, Li M, Anderson BD, Yen L, Stanley D, Mahon C, Kane J, Franks-Skiba K, Cimermancic P, Burlingame A, Sali A, Craik CS, Harris RS, Gross JD, Krogan NJ

A reverse binding motif that contributes to specific protease inhibition by antibodies.

Journal of molecular biology

Schneider EL, Lee MS, Baharuddin A, Goetz DH, Farady CJ, Ward M, Wang CI, Craik CS

Rapid identification of recombinant Fabs that bind to membrane proteins.

Methods (San Diego, Calif.)

Kim J, Stroud RM, Craik CS

Inhibition of Granzyme B by PI-9 protects prostate cancer cells from apoptosis.

The Prostate

Ray M, Hostetter DR, Loeb CR, Simko J, Craik CS

Human and mouse granzyme M display divergent and species-specific substrate specificities.

The Biochemical journal

de Poot SA, Westgeest M, Hostetter DR, Van Damme P, Plasman K, Demeyer K, Broekhuizen R, Gevaert K, Craik CS, Bovenschen N

Inhibitors of SARS-CoV entry--identification using an internally-controlled dual envelope pseudovirion assay.

Antiviral research

Zhou Y, Agudelo J, Lu K, Goetz DH, Hansell E, Chen YT, Roush WR, McKerrow J, Craik CS, Amberg SM, Simmons G

IrCL1 - the haemoglobinolytic cathepsin L of the hard tick, Ixodes ricinus.

International journal for parasitology

Franta Z, Sojka D, Frantova H, Dvorak J, Horn M, Srba J, Talacko P, Mares M, Schneider E, Craik CS, McKerrow JH, Caffrey CR, Kopacek P

GPS-Prot: a web-based visualization platform for integrating host-pathogen interaction data.

BMC bioinformatics

Fahey ME, Bennett MJ, Mahon C, Jäger S, Pache L, Kumar D, Shapiro A, Rao K, Chanda SK, Craik CS, Frankel AD, Krogan NJ

Enzyme inhibition by allosteric capture of an inactive conformation.

Journal of molecular biology

Lee GM, Shahian T, Baharuddin A, Gable JE, Craik CS

Proteases as therapeutics.

The Biochemical journal

Craik CS, Page MJ, Madison EL

Peptide length and leaving-group sterics influence potency of peptide phosphonate protease inhibitors.

Chemistry & biology

Brown CM, Ray M, Eroy-Reveles AA, Egea P, Tajon C, Craik CS

Mechanisms of macromolecular protease inhibitors.

Chembiochem : a European journal of chemical biology

Farady CJ, Craik CS

The oligopeptidase B of Leishmania regulates parasite enolase and immune evasion.

The Journal of biological chemistry

Swenerton RK, Zhang S, Sajid M, Medzihradszky KF, Craik CS, Kelly BL, McKerrow JH

Biochemical properties of a novel cysteine protease of Plasmodium vivax, vivapain-4.

PLoS neglected tropical diseases

Na BK, Bae YA, Zo YG, Choe Y, Kim SH, Desai PV, Avery MA, Craik CS, Kim TS, Rosenthal PJ, Kong Y

How immune peptidases change specificity: cathepsin G gained tryptic function but lost efficiency during primate evolution.

Journal of immunology (Baltimore, Md. : 1950)

Raymond WW, Trivedi NN, Makarova A, Ray M, Craik CS, Caughey GH

Characterization of proteinases from the midgut of Rhipicephalus (Boophilus) microplus involved in the generation of antimicrobial peptides.

Parasites & vectors

Cruz CE, Fogaça AC, Nakayasu ES, Angeli CB, Belmonte R, Almeida IC, Miranda A, Miranda MT, Tanaka AS, Braz GR, Craik CS, Schneider E, Caffrey CR, Daffre S

Prediction of protease substrates using sequence and structure features.

Bioinformatics (Oxford, England)

Barkan DT, Hostetter DR, Mahrus S, Pieper U, Wells JA, Craik CS, Sali A

Antagonistic anti-urokinase plasminogen activator receptor (uPAR) antibodies significantly inhibit uPAR-mediated cellular signaling and migration.

The Journal of biological chemistry

Duriseti S, Goetz DH, Hostetter DR, LeBeau AM, Wei Y, Craik CS

A novel Entamoeba histolytica cysteine proteinase, EhCP4, is key for invasive amebiasis and a therapeutic target.

The Journal of biological chemistry

He C, Nora GP, Schneider EL, Kerr ID, Hansell E, Hirata K, Gonzalez D, Sajid M, Boyd SE, Hruz P, Cobo ER, Le C, Liu WT, Eckmann L, Dorrestein PC, Houpt ER, Brinen LS, Craik CS, Roush WR, McKerrow J, Reed SL

Analysis of an engineered plasma kallikrein inhibitor and its effect on contact activation.

Biological chemistry

Stoop AA, Joshi RV, Eggers CT, Craik CS

Mycobacterium tuberculosis MycP1 protease plays a dual role in regulation of ESX-1 secretion and virulence.

Cell host & microbe

Ohol YM, Goetz DH, Chan K, Shiloh MU, Craik CS, Cox JS

Time-resolved single-step protease activity quantification using nanoplasmonic resonator sensors.

ACS nano

Sun C, Su KH, Valentine J, Rosa-Bauza YT, Ellman JA, Elboudwarej O, Mukherjee B, Craik CS, Shuman MA, Chen FF, Zhang X

Tumor detection by imaging proteolytic activity.

Cancer research

Darragh MR, Schneider EL, Lou J, Phojanakong PJ, Farady CJ, Marks JD, Hann BC, Craik CS

Local protease signaling contributes to neural tube closure in the mouse embryo.

Developmental cell

Camerer E, Barker A, Duong DN, Ganesan R, Kataoka H, Cornelissen I, Darragh MR, Hussain A, Zheng YW, Srinivasan Y, Brown C, Xu SM, Regard JB, Lin CY, Craik CS, Kirchhofer D, Coughlin SR

Continuous imaging of plasmon rulers in live cells reveals early-stage caspase-3 activation at the single-molecule level.

Proceedings of the National Academy of Sciences of the United States of America

Jun YW, Sheikholeslami S, Hostetter DR, Tajon C, Craik CS, Alivisatos AP

Engineering ecotin for identifying proteins with a trypsin fold.

Applied biochemistry and biotechnology

Sathler PC, Craik CS, Takeuchi T, Zingali RB, Castro HC

Inhibition of a viral enzyme by a small-molecule dimer disruptor.

Nature chemical biology

Shahian T, Lee GM, Lazic A, Arnold LA, Velusamy P, Roels CM, Guy RK, Craik CS

Vinyl sulfones as antiparasitic agents and a structural basis for drug design.

The Journal of biological chemistry

Kerr ID, Lee JH, Farady CJ, Marion R, Rickert M, Sajid M, Pandey KC, Caffrey CR, Legac J, Hansell E, McKerrow JH, Craik CS, Rosenthal PJ, Brinen LS

Two approaches to discovering and developing new drugs for Chagas disease.

Memorias do Instituto Oswaldo Cruz

McKerrow JH, Doyle PS, Engel JC, Podust LM, Robertson SA, Ferreira R, Saxton T, Arkin M, Kerr ID, Brinen LS, Craik CS

SmCL3, a gastrodermal cysteine protease of the human blood fluke Schistosoma mansoni.

PLoS neglected tropical diseases

Dvorák J, Mashiyama ST, Sajid M, Braschi S, Delcroix M, Schneider EL, McKerrow WH, Bahgat M, Hansell E, Babbitt PC, Craik CS, McKerrow JH, Caffrey CR

Improving the species cross-reactivity of an antibody using computational design.

Bioorganic & medicinal chemistry letters

Farady CJ, Sellers BD, Jacobson MP, Craik CS

Substrate specificity of transthyretin: identification of natural substrates in the nervous system.

The Biochemical journal

Liz MA, Fleming CE, Nunes AF, Almeida MR, Mar FM, Choe Y, Craik CS, Powers JC, Bogyo M, Sousa MM

Trapping moving targets with small molecules.

Science (New York, N.Y.)

Lee GM, Craik CS

Hemoglobin cleavage site-specificity of the Plasmodium falciparum cysteine proteases falcipain-2 and falcipain-3.

PloS one

Subramanian S, Hardt M, Choe Y, Niles RK, Johansen EB, Legac J, Gut J, Kerr ID, Craik CS, Rosenthal PJ

Positional scanning synthetic combinatorial libraries for substrate profiling.

Methods in molecular biology (Clifton, N.J.)

Schneider EL, Craik CS

A parasite cysteine protease is key to host protein degradation and iron acquisition.

The Journal of biological chemistry

O'Brien TC, Mackey ZB, Fetter RD, Choe Y, O'Donoghue AJ, Zhou M, Craik CS, Caffrey CR, McKerrow JH

Inhibition of a secreted glutamic peptidase prevents growth of the fungus Talaromyces emersonii.

The Journal of biological chemistry

O'Donoghue AJ, Mahon CS, Goetz DH, O'Malley JM, Gallagher DM, Zhou M, Murray PG, Craik CS, Tuohy MG

The functional expression and characterisation of a cysteine peptidase from the invasive stage of the neuropathogenic schistosome Trichobilharzia regenti.

International journal for parasitology

Dolecková K, Kasný M, Mikes L, Cartwright J, Jedelský P, Schneider EL, Dvorák J, Mountford AP, Craik CS, Horák P

Characterization of a cysteine protease from Tritrichomonas foetus that induces host-cell apoptosis.

Archives of biochemistry and biophysics

Lucas JJ, Hayes GR, Kalsi HK, Gilbert RO, Choe Y, Craik CS, Singh BN

Structures and specificity of the human kallikrein-related peptidases KLK 4, 5, 6, and 7.

Biological chemistry

Debela M, Beaufort N, Magdolen V, Schechter NM, Craik CS, Schmitt M, Bode W, Goettig P

Structure of an Fab-protease complex reveals a highly specific non-canonical mechanism of inhibition.

Journal of molecular biology

Farady CJ, Egea PF, Schneider EL, Darragh MR, Craik CS

Identification of the major cysteine protease of Giardia and its role in encystation.

The Journal of biological chemistry

DuBois KN, Abodeely M, Sakanari J, Craik CS, Lee M, McKerrow JH, Sajid M

Using specificity to strategically target proteases.

Bioorganic & medicinal chemistry

Lim MD, Craik CS

MT-SP1 proteolysis and regulation of cell-microenvironment interactions.

Frontiers in bioscience : a journal and virtual library

Darragh MR, Bhatt AS, Craik CS

Structural and functional relationships in the virulence-associated cathepsin L proteases of the parasitic liver fluke, Fasciola hepatica.

The Journal of biological chemistry

Stack CM, Caffrey CR, Donnelly SM, Seshaadri A, Lowther J, Tort JF, Collins PR, Robinson MW, Xu W, McKerrow JH, Craik CS, Geiger SR, Marion R, Brinen LS, Dalton JP

Substrate modulation of enzyme activity in the herpesvirus protease family.

Journal of molecular biology

Lazic A, Goetz DH, Nomura AM, Marnett AB, Craik CS

Hip is a pro-survival substrate of granzyme B.

The Journal of biological chemistry

Hostetter DR, Loeb CR, Chu F, Craik CS

Substrate specificity profiling and identification of a new class of inhibitor for the major protease of the SARS coronavirus.


Goetz DH, Choe Y, Hansell E, Chen YT, McDowell M, Jonsson CB, Roush WR, McKerrow J, Craik CS

Peptide-nanoparticle hybrid SERS probes for optical detection of protease activity.

Journal of nanoscience and nanotechnology

Liu GL, Rosa-Bauza YT, Salisbury CM, Craik C, Ellman JA, Chen FF, Lee LP

Use of recombinant Entamoeba histolytica cysteine proteinase 1 to identify a potent inhibitor of amebic invasion in a human colonic model.

Eukaryotic cell

Meléndez-López SG, Herdman S, Hirata K, Choi MH, Choe Y, Craik C, Caffrey CR, Hansell E, Chávez-Munguía B, Chen YT, Roush WR, McKerrow J, Eckmann L, Guo J, Stanley SL, Reed SL

The mechanism of inhibition of antibody-based inhibitors of membrane-type serine protease 1 (MT-SP1).

Journal of molecular biology

Farady CJ, Sun J, Darragh MR, Miller SM, Craik CS

Coordinate expression and functional profiling identify an extracellular proteolytic signaling pathway.

Proceedings of the National Academy of Sciences of the United States of America

Bhatt AS, Welm A, Farady CJ, Vásquez M, Wilson K, Craik CS

IrAE: an asparaginyl endopeptidase (legumain) in the gut of the hard tick Ixodes ricinus.

International journal for parasitology

Sojka D, Hajdusek O, Dvorák J, Sajid M, Franta Z, Schneider EL, Craik CS, Vancová M, Buresová V, Bogyo M, Sexton KB, McKerrow JH, Caffrey CR, Kopácek P

Isotope-coded and affinity-tagged cross-linking (ICATXL): an efficient strategy to probe protein interaction surfaces.

Journal of the American Chemical Society

Chu F, Mahrus S, Craik CS, Burlingame AL

Expression and characterization of constitutively active human caspase-14.

Biochemical and biophysical research communications

Park K, Kuechle MK, Choe Y, Craik CS, Lawrence OT, Presland RB

Plasminogen activation independent of uPA and tPA maintains wound healing in gene-deficient mice.

The EMBO journal

Lund LR, Green KA, Stoop AA, Ploug M, Almholt K, Lilla J, Nielsen BS, Christensen IJ, Craik CS, Werb Z, Danø K, Rømer J

Specificity profiling of seven human tissue kallikreins reveals individual subsite preferences.

The Journal of biological chemistry

Debela M, Magdolen V, Schechter N, Valachova M, Lottspeich F, Craik CS, Choe Y, Bode W, Goettig P

Ecotin modulates thrombin activity through exosite-2 interactions.

The international journal of biochemistry & cell biology

Castro HC, Monteiro RQ, Assafim M, Loureiro NI, Craik C, Zingali RB

Conversion of trypsin to a functional threonine protease.

Protein science : a publication of the Protein Society

Baird TT, Wright WD, Craik CS

One functional switch mediates reversible and irreversible inactivation of a herpesvirus protease.


Nomura AM, Marnett AB, Shimba N, Dötsch V, Craik CS

Substrate profiling of cysteine proteases using a combinatorial peptide library identifies functionally unique specificities.

The Journal of biological chemistry

Choe Y, Leonetti F, Greenbaum DC, Lecaille F, Bogyo M, Brömme D, Ellman JA, Craik CS

Induced structure of a helical switch as a mechanism to regulate enzymatic activity.

Nature structural & molecular biology

Nomura AM, Marnett AB, Shimba N, Dötsch V, Craik CS

Hepatocyte growth factor is a preferred in vitro substrate for human hepsin, a membrane-anchored serine protease implicated in prostate and ovarian cancers.

The Biochemical journal

Herter S, Piper DE, Aaron W, Gabriele T, Cutler G, Cao P, Bhatt AS, Choe Y, Craik CS, Walker N, Meininger D, Hoey T, Austin RJ

Adhesion signaling by a novel mitotic substrate of src kinases.


Bhatt AS, Erdjument-Bromage H, Tempst P, Craik CS, Moasser MM

Development of alpha-keto-based inhibitors of cruzain, a cysteine protease implicated in Chagas disease.

Bioorganic & medicinal chemistry

Choe Y, Brinen LS, Price MS, Engel JC, Lange M, Grisostomi C, Weston SG, Pallai PV, Cheng H, Hardy LW, Hartsough DS, McMakin M, Tilton RF, Baldino CM, Craik CS

Substrates of the prostate-specific serine protease prostase/KLK4 defined by positional-scanning peptide libraries.

The Prostate

Matsumura M, Bhatt AS, Andress D, Clegg N, Takayama TK, Craik CS, Nelson PS

Optimization of 13C direct detection NMR methods.

Journal of biomolecular NMR

Shimba N, Kovacs H, Stern AS, Nomura AM, Shimada I, Hoch JC, Craik CS, Dötsch V

A multi-enzyme cascade of hemoglobin proteolysis in the intestine of blood-feeding hookworms.

The Journal of biological chemistry

Williamson AL, Lecchi P, Turk BE, Choe Y, Hotez PJ, McKerrow JH, Cantley LC, Sajid M, Craik CS, Loukas A

Methyl groups as probes for proteins and complexes in in-cell NMR experiments.

Journal of the American Chemical Society

Serber Z, Straub W, Corsini L, Nomura AM, Shimba N, Craik CS, Ortiz de Montellano P, Dötsch V

Communication between the active sites and dimer interface of a herpesvirus protease revealed by a transition-state inhibitor.

Proceedings of the National Academy of Sciences of the United States of America

Marnett AB, Nomura AM, Shimba N, Ortiz de Montellano PR, Craik CS

The periplasmic serine protease inhibitor ecotin protects bacteria against neutrophil elastase.

The Biochemical journal

Eggers CT, Murray IA, Delmar VA, Day AG, Craik CS

Identification and biochemical characterization of vivapains, cysteine proteases of the malaria parasite Plasmodium vivax.

The Biochemical journal

Na BK, Shenai BR, Sijwali PS, Choe Y, Pandey KC, Singh A, Craik CS, Rosenthal PJ

Untitled Publication

Brachyurins. Tsu, C., and Craik, C.S. Handbook of Proteolytic Enzymes

Untitled Publication

Shimba, N. Nomura, A.M., Marnett, A.B. and Craik, C.S. Herpesvirus Protease Inhibition by Dimer Disruption. J. Virol

Quantitative identification of the protonation state of histidines in vitro and in vivo.


Shimba N, Serber Z, Ledwidge R, Miller SM, Craik CS, Dötsch V

The oligomeric structure of human granzyme A is a determinant of its extended substrate specificity.

Nature structural biology

Bell JK, Goetz DH, Mahrus S, Harris JL, Fletterick RJ, Craik CS

Catalytic properties and inhibition of proline-specific dipeptidyl peptidases II, IV and VII.

The Biochemical journal

Leiting B, Pryor KD, Wu JK, Marsilio F, Patel RA, Craik CS, Ellman JA, Cummings RT, Thornberry NA

The CD8+ cell noncytotoxic anti-HIV response can be blocked by protease inhibitors.

Proceedings of the National Academy of Sciences of the United States of America

Mackewicz CE, Craik CS, Levy JA

Elimination of 13Calpha splitting in protein NMR spectra by deconvolution with maximum entropy reconstruction.

Journal of the American Chemical Society

Shimba N, Stern AS, Craik CS, Hoch JC, Dötsch V

Quantitation of membrane type serine protease 1 (MT-SP1) in transformed and normal cells.

Biological chemistry

Bhatt AS, Takeuchi T, Ylstra B, Ginzinger D, Albertson D, Shuman MA, Craik CS

Design and synthesis of novel inhibitors of gelatinase B.

Bioorganic & medicinal chemistry letters

Wang X, Choe Y, Craik CS, Ellman JA

Cercarial elastase is encoded by a functionally conserved gene family across multiple species of schistosomes.

The Journal of biological chemistry

Salter JP, Choe Y, Albrecht H, Franklin C, Lim KC, Craik CS, McKerrow JH

Substrate specificity of schistosome versus human legumain determined by P1-P3 peptide libraries.

Molecular and biochemical parasitology

Mathieu MA, Bogyo M, Caffrey CR, Choe Y, Lee J, Chapman H, Sajid M, Craik CS, McKerrow JH

Expedient solid-phase synthesis of fluorogenic protease substrates using the 7-amino-4-carbamoylmethylcoumarin (ACC) fluorophore.

The Journal of organic chemistry

Maly DJ, Leonetti F, Backes BJ, Dauber DS, Harris JL, Craik CS, Ellman JA

Conformational change coupling the dimerization and activation of KSHV protease.


Pray TR, Reiling KK, Demirjian BG, Craik CS

Altered substrate specificity of drug-resistant human immunodeficiency virus type 1 protease.

Journal of virology

Dauber DS, Ziermann R, Parkin N, Maly DJ, Mahrus S, Harris JL, Ellman JA, Petropoulos C, Craik CS

Novel inter-protein cross-link identified in the GGH-ecotin D137Y dimer.

Protein science : a publication of the Protein Society

Person MD, Brown KC, Mahrus S, Craik CS, Burlingame AL

Definition of the extended substrate specificity determinants for beta-tryptases I and II.

The Journal of biological chemistry

Harris JL, Niles A, Burdick K, Maffitt M, Backes BJ, Ellman JA, Kuntz I, Haak-Frendscho M, Craik CS

The role of ecotin dimerization in protease inhibition.

Journal of molecular biology

Eggers CT, Wang SX, Fletterick RJ, Craik CS

A plasma kallikrein-dependent plasminogen cascade required for adipocyte differentiation.

Nature cell biology

Selvarajan S, Lund LR, Takeuchi T, Craik CS, Werb Z

Rapid and general profiling of protease specificity by using combinatorial fluorogenic substrate libraries.

Proceedings of the National Academy of Sciences of the United States of America

Harris JL, Backes BJ, Leonetti F, Mahrus S, Ellman JA, Craik CS

Compromise and accommodation in ecotin, a dimeric macromolecular inhibitor of serine proteases.

Journal of molecular biology

Gillmor SA, Takeuchi T, Yang SQ, Craik CS, Fletterick RJ

Cathepsin G activates protease-activated receptor-4 in human platelets.

The Journal of biological chemistry

Sambrano GR, Huang W, Faruqi T, Mahrus S, Craik C, Coughlin SR

Macromolecular inhibitors of HIV-1 protease. Characterization of designed heterodimers.

The Journal of biological chemistry

Rozzelle JE, Dauber DS, Todd S, Kelley R, Craik CS

HIV protease as a target for retrovirus vector-mediated gene therapy.

Biochimica et biophysica acta

Todd S, Anderson C, Jolly DJ, Craik CS

J. Am. Chem. Soc

Chemically Mediated Site-Specific Cleavage of Proteins

B. Wang, M. Lodder, J. Zhou, T.T. Baird, Jr., K.C. Brown, C.S. Craik, S.M. Hecht

Untitled Publication

K.K. Reiling, T.R. Pray, C.S. Craik, R.M. Stroud. Structure: Regulation of Activity and Dimerization by Conserved Structural Elements. Biochemistry

Untitled Publication

T.T. Baird Jr., B. Wang, M. Lodder, S.M. Hecht and C.S. Craik. Generation of Active Trypsin by Chemical Cleavage. Tetrahedron Letters

Auto-inactivation by cleavage within the dimer interface of Kaposi's sarcoma-associated herpesvirus protease.

Journal of molecular biology

Pray TR, Nomura AM, Pennington MW, Craik CS

Definition and redesign of the extended substrate specificity of granzyme B.

The Journal of biological chemistry

Harris JL, Peterson EP, Hudig D, Thornberry NA, Craik CS

Ecotin: a serine protease inhibitor with two distinct and interacting binding sites.

Journal of molecular biology

Yang SQ, Wang CI, Gillmor SA, Fletterick RJ, Craik CS

Engineering enzyme specificity.

Current opinion in chemical biology

Harris JL, Craik CS

Engineering catalytically defective forms of HIV protease to modulate its activity.

Advances in experimental medicine and biology

Craik CS, Babé LM, Dauber D, McPhee F, Rosé J, Unal A

Optimization of a macromolecular inhibitor of HIV-1 protease.

Advances in experimental medicine and biology

Dauber DS, McPhee F, Unal A, Craik CS

Alkylation of a catalytic aspartate group of the SIV protease by an epoxide inhibitor.

Bioorganic & medicinal chemistry

Caldera PS, Yu Z, Knegtel RM, McPhee F, Burlingame AL, Craik CS, Kuntz ID, Ortiz de Montellano PR

The protease and the assembly protein of Kaposi's sarcoma-associated herpesvirus (human herpesvirus 8).

Journal of virology

Unal A, Pray TR, Lagunoff M, Pennington MW, Ganem D, Craik CS

Structural determinants of specificity in the cysteine protease cruzain.

Protein science : a publication of the Protein Society

Gillmor SA, Craik CS, Fletterick RJ

The discovery, characterization and crystallographically determined binding mode of an FMOC-containing inhibitor of HIV-1 protease.

Bioorganic & medicinal chemistry

Rutenber EE, De Voss JJ, Hoffman L, Stroud RM, Lee KH, Alvarez J, McPhee F, Craik C, Ortiz de Montellano PR

P-4 and RNKP-7, new granzyme-like serine proteases expressed in activated rat lymphocytes.

Journal of immunology (Baltimore, Md. : 1950)

Ewoldt GR, Smyth MJ, Darcy PK, Harris JL, Craik CS, Horowitz B, Woodard SL, Powers JC, Hudig D

Obstruction of HIV-1 particle release by interferon-alpha occurs before viral protease processing and is independent of envelope glycoprotein.

Journal of interferon & cytokine research : the official journal of the International Society for Interferon and Cytokine Research

Babé LM, Unal A, Craik CS

Use of the intestinal bile acid transporter for the uptake of cholic acid conjugates with HIV-1 protease inhibitory activity.

Pharmaceutical research

Kågedahl M, Swaan PW, Redemann CT, Tang M, Craik CS, Szoka FC, Oie S

Untitled Publication

C.S. Craik & R.J. Fletterick. The Marriage of Protein Structure and Pharmaceutical Discovery. Biotech. & Appl. Biochem. 26

Bile pigments as HIV-1 protease inhibitors and their effects on HIV-1 viral maturation and infectivity in vitro.

The Biochemical journal

McPhee F, Caldera PS, Bemis GW, McDonagh AF, Kuntz ID, Craik CS

Engineering human immunodeficiency virus 1 protease heterodimers as macromolecular inhibitors of viral maturation.

Proceedings of the National Academy of Sciences of the United States of America

McPhee F, Good AC, Kuntz ID, Craik CS

Three-dimensional structures of HIV-1 and SIV protease product complexes.


Rose RB, Craik CS, Douglas NL, Stroud RM

X-ray structures of a designed binding site in trypsin show metal-dependent geometry.


Brinen LS, Willett WS, Craik CS, Fletterick RJ

Substrate recognition by recombinant serine collagenase 1 from Uca pugilator.

The Journal of biological chemistry

Tsu CA, Craik CS

Isolation and characterization of two cDNAs from Atlantic cod encoding two distinct psychrophilic elastases.

Comparative biochemistry and physiology. Part B, Biochemistry & molecular biology

Gudmundsdóttir E, Spilliaert R, Yang Q, Craik CS, Bjarnason JB, Gudmundsdóttir A

Phage display of proteases and macromolecular inhibitors.

Methods in enzymology

Wang CI, Yang Q, Craik CS

Untitled Publication

E.E. Rutenber, F. McPhee, A.P. Kaplan, S.L. Gallion, J.C. Hogan Jr., C.S. Craik & R.M. Stroud. A New Class of HIV1 Protease Inhibitor: The Crystallographic Structure, Inhibition and Chemical Synthesis of an Aminimide Peptide Isostere. Bioorg.& Med. Chem. 4

Untitled Publication

R. Li, X. Chen, B. Gong, Z. Li, E. Davidson, G. Kurzban, R.E. Miller, E.O. Nuzman, J.H. McKerrow, R.J. Fletterick, S.A. Gillmore, C.S. Craik, I.D. Kuntz, F.E. Cohen & G.L. Kenyon. Structure-based Design of Parasitic Protease Inhibitors. Bioorg. & Med. Chem. 4

Untitled Publication

S. Halfon & C.S. Craik. Regulation of Proteolytic Activity by Engineered Tridentate Metal Binding Loops. J. Am. Chem. Soc. 118

Untitled Publication

W.S. Willett, L.S. Brinen, R.J. Fletterick & C.S. Craik. Delocalizing Trypsin Specificity with Metal-Activation. Biochem; 35

Untitled Publication

Z. Yu, P. Caldera, F. McPhee, J. DeVoss, P.R. Jones, A. Burlingame, I. Kuntz, C.S. Craik & P.R. Ortiz de Montellano. Irreversible Inhibition of the HIV-1 Protease: Targeting Alkylating Agents to the Catalytic Aspartate Groups. J. Amer. Chem. Soc. 118

Trans-dominant inhibitory human immunodeficiency virus type 1 protease monomers prevent protease activation and virion maturation.

Proceedings of the National Academy of Sciences of the United States of America

Babé LM, Rosé J, Craik CS

Trypsin specificity increased through substrate-assisted catalysis.


Corey DR, Willett WS, Coombs GS, Craik CS

The crystal structure of cruzain: a therapeutic target for Chagas' disease.

Journal of molecular biology

McGrath ME, Eakin AE, Engel JC, McKerrow JH, Craik CS, Fletterick RJ

Structural basis of substrate specificity in the serine proteases.

Protein science : a publication of the Protein Society

Perona JJ, Craik CS

Engineered metal regulation of trypsin specificity.


Willett WS, Gillmor SA, Perona JJ, Fletterick RJ, Craik CS

Untitled Publication

A.E. Eakin, J.H. McKerrow & C.S.Craik. A Cysteine Protease is a Target for the Enzyme Structure-based Design of Antiparasitic Drugs. Drug Information Journal 29

Structure-assisted design of nonpeptide human immunodeficiency virus-1 protease inhibitors.

American journal of respiratory and critical care medicine

Rosé JR, Craik CS

Atlantic cod cDNA encoding a psychrophilic chymotrypsinogen.

Biochimica et biophysica acta

Guthmundsdóttir A, Oskarsson S, Eakin AE, Craik CS, Bjarnason JB

The substrate specificity of Uca pugilator collagenolytic serine protease 1 correlates with the bovine type I collagen cleavage sites.

The Journal of biological chemistry

Tsu CA, Perona JJ, Schellenberger V, Turck CW, Craik CS

Can small cyclic peptides have the activity and specificity of proteolytic enzymes?

Proceedings of the National Academy of Sciences of the United States of America

Matthews BW, Craik CS, Neurath H

In vitro characterization of nonpeptide irreversible inhibitors of HIV proteases.

The Journal of biological chemistry

Salto R, Babé LM, Li J, Rosé JR, Yu Z, Burlingame A, De Voss JJ, Sui Z, Ortiz de Montellano P, Craik CS

Exogenous acetate reconstitutes the enzymatic activity of trypsin Asp189Ser.


Perona JJ, Hedstrom L, Wagner RL, Rutter WJ, Craik CS, Fletterick RJ

Haloperidol-based irreversible inhibitors of the HIV-1 and HIV-2 proteases.

Journal of medicinal chemistry

De Voss JJ, Sui Z, DeCamp DL, Salto R, Babé LM, Craik CS, Ortiz de Montellano PR

Untitled Publication

K.L. Lee, F. McPhee, J.J. DeVoss, C.S. Craik & P. Ortiz de Montellano. Nonpeptide HIV Protease Inhibitors. Differential Introduction of Alkylamino Groups into the two Aryl Rings of Haloperidol. J. of Organic Chemistry 59

Isolation and characterization of cDNAs from Atlantic cod encoding two different forms of trypsinogen.

European journal of biochemistry

Gudmundsdóttir A, Gudmundsdóttir E, Oskarsson S, Bjarnason JB, Eakin AK, Craik CS

Locating the catalytic water molecule in serine proteases.

Science (New York, N.Y.)

Perona JJ, Craik CS, Fletterick RJ

Trypsin display on the surface of bacteriophage.


Corey DR, Shiau AK, Yang Q, Janowski BA, Craik CS

Crystal structures of rat anionic trypsin complexed with the protein inhibitors APPI and BPTI.

Journal of molecular biology

Perona JJ, Tsu CA, Craik CS, Fletterick RJ

Production of crystallizable cruzain, the major cysteine protease from Trypanosoma cruzi.

The Journal of biological chemistry

Eakin AE, McGrath ME, McKerrow JH, Fletterick RJ, Craik CS

Structure of an engineered, metal-actuated switch in trypsin.


McGrath ME, Haymore BL, Summers NL, Craik CS, Fletterick RJ

J. Bio. Chem

Structure of a Non-Peptide Inhibitor Complexed with HIV-1 Protease: Developing a Cycle of Structure-Based Drug Design

E. Rutenber, E.B. Fauman, R.J. Keenan, S. Fong, P.S. Furth, P.R. Ortiz de Montellano, E. Meng, I.D. Kuntz, D.L. DeCamp, R. Salto, J.R. Rosé, C.S. Craik, R.M. Stroud.


Synthesis of Haloperidol Ethanedithioketal HIV-1 Protease Inhibitors: Magnesium Chloride Facilitated Addition of Grignard Reagents

Z. Sui, J. DeVoss, D. DeCamp, J. Li, C.S. Craik & P.R. Ortiz de Montellano

Untitled Publication

D.L. Decamp, S.B. Kahl & C.S. Craik. Boronated Porphyrins—A New Class of HIV Proteinase Inhibitors. Intl. Antiviral News 1

Untitled Publication

J.J. Perona, C.A. Tsu, M.E. McGrath, C.S. Craik & R.J. Fletterick. Relocating a Negative Charge in the Binding Pocket of Trypsin. J. Mol. Bio. 230

Untitled Publication

T.K. Sawyer, J.F. Fisher, J.B. Hester, C.W. Smith, A.G. Tomasselli, W.G. Tarpley, P.S. Burton, J.O. Hui T.J. McQuade, R.A. Conradi, V.S. Bradford, L. Liu, J.H. Kinner, J.Tustin,D.L. Alexander, A.W. Harrison, D.E. Emmert, D.J. Staples, L.I. Maggira, Y.Z. Zhang, R.A. Poorman, BM. Dunn, C. Rao, .E. Scarborough, W.T. Lowther, C.S. Craik, D. DeCamp, J.Moon, W.H. Howe & R.L. Heinrikson. Peptidomimetic Inhibitors of Human Immunodeficiency Virus Protease (HIV-PR): Design, Enzyme Binding and Selectivity, Antiviral Efficacy and Cell Permeability Properties. Bioorg. Med. Chem. Letts 3

Untitled Publication

Z. Sui, R. Salto, C.S. Craik, P. Ortiz de Montellano. Inhibition of the HIV1 and the HIV2 Proteases by Curcumin and Curcumin Boron Complexes. Bioorg. & Med. Chem. Let. 1

Synthetic "interface" peptides alter dimeric assembly of the HIV 1 and 2 proteases.

Protein science : a publication of the Protein Society

Babé LM, Rosé J, Craik CS

Specific inhibition of HIV-1 protease by boronated porphyrins.

Journal of medicinal chemistry

DeCamp DL, Babé LM, Salto R, Lucich JL, Koo MS, Kahl SB, Craik CS

The sequence, organization, and expression of the major cysteine protease (cruzain) from Trypanosoma cruzi.

The Journal of biological chemistry

Eakin AE, Mills AA, Harth G, McKerrow JH, Craik CS

Perturbing the polar environment of Asp102 in trypsin: consequences of replacing conserved Ser214.


McGrath ME, Vásquez JR, Craik CS, Yang AS, Honig B, Fletterick RJ

Engineered metalloregulation in enzymes.

Trends in biochemical sciences

Higaki JN, Fletterick RJ, Craik CS

Physical map location of the new Escherichia coli gene eco, encoding the serine protease inhibitor ecotin.

Journal of bacteriology

Erpel T, Hwang P, Craik CS, Fletterick RJ, McGrath ME

Int. J. Pep. Protein Res

HIV Protease (HIV PR) Inhibitor Structure-Activity-Selectivity and Active Site Molecular Modeling of High Affinity Leu [CH(OH)CH2] Val Modified Viral and Nonviral Substrate Analogs

T.K. Sawyer, D.J. Staples, L. Liu, A.G. Tomasselli, J.O. Hui, K. O’Connell, H. Schostarez, J.B. Hester, J. Moon, W.J. Howe, C.W. Smith, D. L. DeCamp, C.S. Craik, B.M. Dunn,W. T. Lowther, J. Harris, R.A. Poorman, A. Wlodawer, M. Jaskolski & R.L. Heinrikson.

Untitled Publication

D.R. Corey, M.E. McGrath, J.R. Vasquez, R.J. Fletterick & C.S. Craik. An Alternate Geometry for the Catalytic Triad of Serine Proteases. J. Amer. Chem. Soc. 114

A primary determinant for lipoxygenase positional specificity.


Sloane DL, Leung R, Craik CS, Sigal E

The sequence and reactive site of ecotin. A general inhibitor of pancreatic serine proteases from Escherichia coli.

The Journal of biological chemistry

McGrath ME, Hines WM, Sakanari JA, Fletterick RJ, Craik CS

Inhibition of HIV protease activity by heterodimer formation.


Babé LM, Pichuantes S, Craik CS

A Primary Determinant for Lipoxygenase Postional Specificity. Nature 354, 149-152

A Primary Determinant for Lipoxygenase Postional Specificity. Nature 354, 149-152

D.L. Sloane, R. Leung, C.S. Craik & E. Sigal

Adv. Exptl. Med. Bio

Structure-based inhibition of HIV-1 protease activity and viral infectivity

D.L. DeCamp, L.M. Babé, P. Furth, P. Ortiz de Montellano, I.D. Kuntz & C.S. Craik

Calcium-free calmodulin is a substrate of proteases from human immunodeficiency viruses 1 and 2.


Tomasselli AG, Howe WJ, Hui JO, Sawyer TK, Reardon IM, DeCamp DL, Craik CS, Heinrikson RL

Expression of cloned human 15-lipoxygenase in eukaryotic and prokaryotic systems.

Advances in prostaglandin, thromboxane, and leukotriene research

Sloane DL, Dixon RA, Craik CS, Sigal E

Structure-based inhibition of HIV-1 protease activity and viral infectivity.

Advances in experimental medicine and biology

DeCamp DL, Babé LM, Furth P, Ortiz de Montellano P, Kuntz ID, Craik CS

Time dependent heterodimer formation leads to inhibition of HIV protease activity.

Advances in experimental medicine and biology

Babé LM, Craik CS

Untitled Publication

C.S.Craik. Modus Operandi. Nature

Regulation of serine protease activity by an engineered metal switch.


Higaki JN, Haymore BL, Chen S, Fletterick RJ, Craik CS

Characterization of the human immunodeficiency virus type-1 reverse transcriptase enzyme produced in yeast.

Biochemical and biophysical research communications

Bathurst IC, Moen LK, Lujan MA, Gibson HL, Feucht PH, Pichuantes S, Craik CS, Santi DV, Barr PJ

Homeodomain of yeast repressor alpha 2 contains a nuclear localization signal.

Proceedings of the National Academy of Sciences of the United States of America

Hall MN, Craik C, Hiraoka Y

Structure-based design of nonpeptide inhibitors specific for the human immunodeficiency virus 1 protease.

Proceedings of the National Academy of Sciences of the United States of America

DesJarlais RL, Seibel GL, Kuntz ID, Furth PS, Alvarez JC, Ortiz de Montellano PR, DeCamp DL, Babé LM, Craik CS

Recombinant HIV2 protease processes HIV1 Pr53gag and analogous junction peptides in vitro.

The Journal of biological chemistry

Pichuantes S, Babé LM, Barr PJ, DeCamp DL, Craik CS

Human mast cell tryptase: multiple cDNAs and genes reveal a multigene serine protease family.

Proceedings of the National Academy of Sciences of the United States of America

Vanderslice P, Ballinger SM, Tam EK, Goldstein SM, Craik CS, Caughey GH

Human carboxypeptidase A identifies a BglII RFLP and maps to 7q31-qter.

American journal of human genetics

Stewart EA, Craik CS, Hake L, Bowcock AM

Expression of cloned human reticulocyte 15-lipoxygenase and immunological evidence that 15-lipoxygenases of different cell types are related.

The Journal of biological chemistry

Sigal E, Grunberger D, Highland E, Gross C, Dixon RA, Craik CS

Amplification and sequencing of genomic DNA fragments encoding cysteine proteases from protozoan parasites.

Molecular and biochemical parasitology

Eakin AE, Bouvier J, Sakanari JA, Craik CS, McKerrow JH

The expression of active human reticulocyte 15-lipoxygenase in bacteria.

Biomedica biochimica acta

Sloane DL, Craik CS, Sigal E

Untitled Publication

L. Evnin, J. Vasquez & C.S. Craik. Proc. Substrate Specificity of Trypsin Investigated Using a Genetic Selection. Natl. Acad. Sci. USA 87

Untitled Publication

A.L. Ferris, A. Hizi, S.D. Showalter, S. Pichuantes, L. Babé & C.S. Craik. Immunologic and Proteolytic Analysis of HIV-2 Reverse Transcriptase Structure. Virology 175

Untitled Publication

E. Stewart, C.S. Craik, L. Hake & A. Bowcock. Human CPA Identifies a BglII RFLP and Maps to 7q31-qter. Amer. J. Hum. Gen. 46, 795 -800

Untitled Publication

M. Obukowicz, M. Gustafson, K. Junger, R. Leimgruber, A. Wittwer, T-C. Wun, T. Warren, B. Bishop, K. Mathis, D. McPherson, N. Siegel, M. Jennings, B. Brightwell, J. Diaz-Collier, L. Bell, C.S. Craik & W. Tacon. Secretion of Active Kringle 2-Serine Protease in E. coli. J. Bio. Chem. 29, 9737-9745

Untitled Publication

S. Pichuantes, L. Babé, P. Barr, D. DeCamp & C.S. Craik. Recombinant HIV 2 Protease Processes HIV 1 Pr53gag and Analogous Junction Peptides In Vitro. J. Bio. Chem. 265, 13890-13898

Crystal structures of two engineered thiol trypsins.


McGrath ME, Wilke ME, Higaki JN, Craik CS, Fletterick RJ

Serine proteases from nematode and protozoan parasites: isolation of sequence homologs using generic molecular probes.

Proceedings of the National Academy of Sciences of the United States of America

Sakanari JA, Staunton CE, Eakin AE, Craik CS, McKerrow JH

An expression system for trypsin.

Journal of cellular biochemistry

Vasquez JR, Evnin LB, Higaki JN, Craik CS

Rapid preparation of proteins for crystallization trials.


McGrath ME, Fletterick RJ, Craik CS

[A case of aseptic meningoencephalitis with recurrent abnormal behavior, status epilepticus and aphthous stomatitis, improved by acyclovir].

Rinsho shinkeigaku = Clinical neurology

Shimada K, Koh CS, Hashimoto T, Shoji S, Yanagisawa N

Arachidonate 15-lipoxygenase from human leukocytes: purification and structural homology to other mammalian lipoxygenases.

Advances in prostaglandin, thromboxane, and leukotriene research

Sigal E, Grunberger D, Craik CS, Caughey GH, Nadel JA

Cloning and expression of human arachidonate 15-lipoxygenase.

Transactions of the Association of American Physicians

Sigal E, Craik CS, Dixon RA, Nadel JA

Untitled Publication

A. Eakin, J.N. Higaki, J.H. McKerrow & C.S. Craik. Cysteine or Serine Proteinase. Nature 342,132

Untitled Publication

J. Higaki L.B. Evnin & C.S. Craik. Introduction of a Cysteine Protease Active Site into Trypsin. Biochem. 28, 9256-9263

Molecular cloning and primary structure of human 15-lipoxygenase.

Biochemical and biophysical research communications

Sigal E, Craik CS, Highland E, Grunberger D, Costello LL, Dixon RA, Nadel JA

Structural and functional integrity of specificity and catalytic sites of trypsin.

International journal of peptide and protein research

Gráf L, Hegyi G, Likó I, Hepp J, Medzihradszky K, Craik CS, Rutter WJ

A novel rat carboxypeptidase, CPA2: characterization, molecular cloning, and evolutionary implications on substrate specificity in the carboxypeptidase gene family.

The Journal of biological chemistry

Gardell SJ, Craik CS, Clauser E, Goldsmith EJ, Stewart CB, Graf M, Rutter WJ

Structural characterization of the rat carboxypeptidase A1 and B genes. Comparative analysis of the rat carboxypeptidase gene family.

The Journal of biological chemistry

Clauser E, Gardell SJ, Craik CS, MacDonald RJ, Rutter WJ

Efficient targeting to storage granules of human proinsulins with altered propeptide domain.

The Journal of cell biology

Powell SK, Orci L, Craik CS, Moore HP

Arachidonate 15-lipoxygenase from human eosinophil-enriched leukocytes: partial purification and properties.

Biochemical and biophysical research communications

Sigal E, Grunberger D, Cashman JR, Craik CS, Caughey GH, Nadel JA

Studies of specificity and catalysis in trypsin by structural analysis of site-directed mutants.

Critical reviews in biotechnology

Sprang SR, Fletterick RJ, Gráf L, Rutter WJ, Craik CS

The catalytic role of the active site aspartic acid in serine proteases.

Science (New York, N.Y.)

Craik CS, Roczniak S, Largman C, Rutter WJ

The three-dimensional structure of Asn102 mutant of trypsin: role of Asp102 in serine protease catalysis.

Science (New York, N.Y.)

Sprang S, Standing T, Fletterick RJ, Stroud RM, Finer-Moore J, Xuong NH, Hamlin R, Rutter WJ, Craik CS

Isolation and characterization of a cDNA encoding rat cationic trypsinogen.


Fletcher TS, Alhadeff M, Craik CS, Largman C

Redesigning trypsin via genetic engineering.

Journal of cellular biochemistry

Craik CS, Roczniak S, Sprang S, Fletterick R, Rutter W

Replacement of lysine residue 1030 in the putative ATP-binding region of the insulin receptor abolishes insulin- and antibody-stimulated glucose uptake and receptor kinase activity.

Proceedings of the National Academy of Sciences of the United States of America

Ebina Y, Araki E, Taira M, Shimada F, Mori M, Craik CS, Siddle K, Pierce SB, Roth RA, Rutter WJ

Evolution of catalysis in the serine proteases.

Cold Spring Harbor symposia on quantitative biology

Higaki JN, Gibson BW, Craik CS

Untitled Publication

C.S. Craik, S. Roczniak, S. Sprang, R.J. Fletterick & W.J. Rutter. Edited by D. Cunningham and G. Long. New York: Alan R Liss, Inc. Redesigning Trypsin via Genetic Engineering. In: Proteases in Biological Control and Biotechnology

Untitled Publication

C.S. Craik. Edited by D. Oxender. New York: Alan R. Liss, Inc. Expression and Overproduction of Proteins. In: Protein Structure, Folding and Design 2, pp. 467-476.

Untitled Publication

T.L. Burgess, C.S. Craik, L. Matsuuchi & R.B. Kelly. In Vitro Mutagenesis of Trypsinogen: The Role of the N-Terminus in Intracellular Protein Targeting to Secretory Granules. J. Cell Bio. 105, 659-668

Untitled Publication

W.J. Rutter, S.J. Gardell, S. Roczniak, D. Hilvert, S. Sprang, R.J. Fletterick & C.S. Craik. Edited by D. Oxender and C.F. Fox. New York: Alan R. Liss, Inc. Redesigning Proteins via Genetic Engineering. In: Protein Modification and Design, pp. 257-267

Genetic analysis of cystic fibrosis: linkage of DNA and classical markers in multiplex families.

American journal of human genetics

Bowcock AM, Crandall J, Daneshvar L, Lee GM, Young B, Zunzunegui V, Craik C, Cavalli-Sforza LL, King MC

Untitled Publication

S. Gardell, C.S. Craik, D. Hilvert, M. Urdea & W. Rutter. Edited by I. Bertini, C. Luchinat, W. Maret, and M. Zeppezauer. Boston, Massachusetts: Birkhäuser. Probing the Role of Tyrosine 248 in Carboxypeptidase A with Site-Directed Mutagenesis. In: Comparative Analysis of Catalytic Mechanisms of Zinc Enzymes.

Redesigning trypsin: alteration of substrate specificity.

Science (New York, N.Y.)

Craik CS, Largman C, Fletcher T, Roczniak S, Barr PJ, Fletterick R, Rutter WJ


Use of Oligonucleotides for Site-Specific Mutagenesis

C.S. Craik

Isolation and sequence of a rat chymotrypsin B gene.

The Journal of biological chemistry

Bell GI, Quinto C, Quiroga M, Valenzuela P, Craik CS, Rutter WJ

Structure of the two related elastase genes expressed in the rat pancreas.

The Journal of biological chemistry

Swift GH, Craik CS, Stary SJ, Quinto C, Lahaie RG, Rutter WJ, MacDonald RJ

Structure of two related rat pancreatic trypsin genes.

The Journal of biological chemistry

Craik CS, Choo QL, Swift GH, Quinto C, MacDonald RJ, Rutter WJ

Chromosomal assignments of genes for trypsin, chymotrypsin B, and elastase in mouse.

Somatic cell and molecular genetics

Honey NK, Sakaguchi AY, Lalley PA, Quinto C, MacDonald RJ, Craik C, Bell GI, Rutter WJ, Naylor SL

Chromosomal assignments of human genes for serine proteases trypsin, chymotrypsin B, and elastase.

Somatic cell and molecular genetics

Honey NK, Sakaguchi AY, Quinto C, MacDonald RJ, Bell GI, Craik C, Rutter WJ, Naylor SL

Splice junctions: association with variation in protein structure.

Science (New York, N.Y.)

Craik CS, Rutter WJ, Fletterick R

Intron-exon splice junctions map at protein surfaces.


Craik CS, Sprang S, Fletterick R, Rutter WJ

Untitled Publication

C.S. Craik & S. Beychok. Edited by C. Ho. In: Interaction Between Iron Proteins in Oxygen and Electron Transport, Elsevier North Holland Biomedical Press

Refolding defects in hemoglobin Rothschild.

The Journal of biological chemistry

Craik CS, Vallette I, Beychok S, Waks M

Characterization of globin domains: heme binding to the central exon product.

Proceedings of the National Academy of Sciences of the United States of America

Craik CS, Buchman SR, Beychok S