Kevan Shokat, PhD

Professor
Cellular Molecular Pharmacology
+1 415 514-0472
Publications: 

A Patient-derived Xenograft Model of Pancreatic Neuroendocrine Tumors Identifies Sapanisertib as a Possible New Treatment for Everolimus-Resistant Tumors.

Molecular cancer therapeutics

Chamberlain CE, German MS, Yang K, Wang J, VanBrocklin H, Regan M, Shokat KM, Ducker GS, Kim GE, Hann B, Donner DB, Warren RS, Venook AP, Bergsland EK, Lee D, Wang Y, Nakakura EK

Type II kinase inhibitors targeting Cys-gatekeeper kinases display orthogonality with wild type and Ala/Gly-gatekeeper kinases.

ACS chemical biology

Ocasio CA, Warkentin AA, McIntyre PJ, Barkovich KJ, Vesely C, Spencer J, Shokat KM, Bayliss R

A High-Throughput Luciferase Assay to Evaluate Proteolysis of the Single-Turnover Protease PCSK9.

Journal of visualized experiments : JoVE

Chorba JS, Galvan AM, Shokat KM

Chemical genetic inhibition of DEAD-box proteins using covalent complementarity.

Nucleic acids research

Barkovich KJ, Moore MK, Hu Q, Shokat KM

Kinome rewiring reveals AURKA limits PI3K-pathway inhibitor efficacy in breast cancer.

Nature chemical biology

Donnella HJ, Webber JT, Levin RS, Camarda R, Momcilovic O, Bayani N, Shah KN, Korkola JE, Shokat KM, Goga A, Gordan JD, Bandyopadhyay S

Comprehensive analysis of T cell leukemia signals reveals heterogeneity in the PI3 kinase-Akt pathway and limitations of PI3 kinase inhibitors as monotherapy.

PloS one

Ksionda O, Mues M, Wandler AM, Donker L, Tenhagen M, Jun J, Ducker GS, Matlawska-Wasowska K, Shannon K, Shokat KM, Roose JP

Novel K-Ras G12C Switch-II Covalent Binders Destabilize Ras and Accelerate Nucleotide Exchange.

Journal of chemical information and modeling

Nnadi CI, Jenkins ML, Gentile DR, Bateman LA, Zaidman D, Balius TE, Nomura DK, Burke JE, Shokat KM, London N

Ras Binder Induces a Modified Switch-II Pocket in GTP and GDP States.

Cell chemical biology

Gentile DR, Rathinaswamy MK, Jenkins ML, Moss SM, Siempelkamp BD, Renslo AR, Burke JE, Shokat KM

Inhibition of Calcium Dependent Protein Kinase 1 (CDPK1) by Pyrazolopyrimidine Analogs Decreases Establishment and Reoccurrence of Central Nervous System Disease by Toxoplasma gondii.

Journal of medicinal chemistry

Rutaganira FU, Barks J, Dhason MS, Wang Q, Lopez MS, Long S, Radke JB, Jones NG, Maddirala AR, Janetka JW, El Bakkouri M, Hui R, Shokat KM, Sibley LD

A new generation of mTORC1 inhibitor attenuates alcohol intake and reward in mice.

Addiction biology

Morisot N, Novotny CJ, Shokat KM, Ron D

Drugging the 'undruggable' cancer targets.

Nature reviews. Cancer

Dang CV, Reddy EP, Shokat KM, Soucek L

Expanding the Scope of Electrophiles Capable of Targeting K-Ras Oncogenes.

Biochemistry

McGregor LM, Jenkins ML, Kerwin C, Burke JE, Shokat KM

Drugging the catalytically inactive state of RET kinase in RET-rearranged tumors.

Science translational medicine

Plenker D, Riedel M, Brägelmann J, Dammert MA, Chauhan R, Knowles PP, Lorenz C, Keul M, Bührmann M, Pagel O, Tischler V, Scheel AH, Schütte D, Song Y, Stark J, Mrugalla F, Alber Y, Richters A, Engel J, Leenders F, Heuckmann JM, Wolf J, Diebold J, Pall G, Peifer M, Aerts M, Gevaert K, Zahedi RP, Buettner R, Shokat KM, McDonald NQ, Kast SM, Gautschi O, Thomas RK, Sos ML

Site-specific incorporation of phosphotyrosine using an expanded genetic code.

Nature chemical biology

Hoppmann C, Wong A, Yang B, Li S, Hunter T, Shokat KM, Wang L

Ablation of PI3K blocks BCR-ABL leukemogenesis in mice, and a dual PI3K/mTOR inhibitor prevents expansion of human BCR-ABL+ leukemia cells.

The Journal of clinical investigation

Kharas MG, Janes MR, Scarfone VM, Lilly MB, Knight ZA, Shokat KM, Fruman DA

Discovery of nitrate-CPK-NLP signalling in central nutrient-growth networks.

Nature

Liu KH, Niu Y, Konishi M, Wu Y, Du H, Sun Chung H, Li L, Boudsocq M, McCormack M, Maekawa S, Ishida T, Zhang C, Shokat K, Yanagisawa S, Sheen J

Long-term oral kinetin does not protect against a-synuclein-induced neurodegeneration in rodent models of Parkinson's disease.

Neurochemistry international

Orr AL, Rutaganira FU, de Roulet D, Huang EJ, Hertz NT, Shokat KM, Nakamura K

A Kinase Inhibitor Targeted to mTORC1 Drives Regression in Glioblastoma.

Cancer cell

Fan Q, Aksoy O, Wong RA, Ilkhanizadeh S, Novotny CJ, Gustafson WC, Truong AY, Cayanan G, Simonds EF, Haas-Kogan D, Phillips JJ, Nicolaides T, Okaniwa M, Shokat KM, Weiss WA

An Optimized Chromatographic Strategy for Multiplexing In Parallel Reaction Monitoring Mass Spectrometry: Insights from Quantitation of Activated Kinases.

Molecular & cellular proteomics : MCP

Urisman A, Levin RS, Gordan JD, Webber JT, Hernandez H, Ishihama Y, Shokat KM, Burlingame AL

Endosomal Phosphatidylinositol 3-Kinase Is Essential for Canonical GPCR Signaling.

Molecular pharmacology

Uchida Y, Rutaganira FU, Jullié D, Shokat KM, von Zastrow M

Overcoming resistance to HER2 inhibitors through state-specific kinase binding.

Nature chemical biology

Novotny CJ, Pollari S, Park JH, Lemmon MA, Shen W, Shokat KM

From Powerful Review Articles to Research Breakthroughs.

Cell chemical biology

Kostic M, Crews CM, Hertweck C, Shokat K, Suga H

Inhibition of Carbonyl Reductase 1 Safely Improves the Efficacy of Doxorubicin in Breast Cancer Treatment.

Antioxidants & redox signaling

Jo A, Choi TG, Jo YH, Jyothi KR, Nguyen MN, Kim JH, Lim S, Shahid M, Akter S, Lee S, Lee KH, Kim W, Cho H, Lee J, Shokat KM, Yoon KS, Kang I, Ha J, Kim SS

Innate immunity kinase TAK1 phosphorylates Rab1 on a hotspot for posttranslational modifications by host and pathogen.

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

Levin RS, Hertz NT, Burlingame AL, Shokat KM, Mukherjee S

Synthetic Lethal Targeting of ARID1A-Mutant Ovarian Clear Cell Tumors with Dasatinib.

Molecular cancer therapeutics

Miller RE, Brough R, Bajrami I, Williamson CT, McDade S, Campbell J, Kigozi A, Rafiq R, Pemberton H, Natrajan R, Joel J, Astley H, Mahoney C, Moore JD, Torrance C, Gordan JD, Webber JT, Levin RS, Shokat KM, Bandyopadhyay S, Lord CJ, Ashworth A

Isocitrate Dehydrogenase Mutations Confer Dasatinib Hypersensitivity and SRC Dependence in Intrahepatic Cholangiocarcinoma.

Cancer discovery

Saha SK, Gordan JD, Kleinstiver BP, Vu P, Najem MS, Yeo JC, Shi L, Kato Y, Levin RS, Webber JT, Damon LJ, Egan RK, Greninger P, McDermott U, Garnett MJ, Jenkins RL, Rieger-Christ KM, Sullivan TB, Hezel AF, Liss AS, Mizukami Y, Goyal L, Ferrone CR, Zhu AX, Joung JK, Shokat KM, Benes CH, Bardeesy N

Overcoming mTOR resistance mutations with a new-generation mTOR inhibitor.

Nature

Rodrik-Outmezguine VS, Okaniwa M, Yao Z, Novotny CJ, McWhirter C, Banaji A, Won H, Wong W, Berger M, de Stanchina E, Barratt DG, Cosulich S, Klinowska T, Rosen N, Shokat KM

Multistep Compositional Remodeling of Supported Lipid Membranes by Interfacially Active Phosphatidylinositol Kinases.

Analytical chemistry

Tabaei SR, Guo F, Rutaganira FU, Vafaei S, Choong I, Shokat KM, Glenn JS, Cho NJ

N-Myc Drives Neuroendocrine Prostate Cancer Initiated from Human Prostate Epithelial Cells.

Cancer cell

Lee JK, Phillips JW, Smith BA, Park JW, Stoyanova T, McCaffrey EF, Baertsch R, Sokolov A, Meyerowitz JG, Mathis C, Cheng D, Stuart JM, Shokat KM, Gustafson WC, Huang J, Witte ON

Our Advisors, Our Ambassadors, Our Editorial Board Members.

Cell chemical biology

Kostic M, Crews CM, Hertweck C, Shokat K, Suga H

Design and Structural Characterization of Potent and Selective Inhibitors of Phosphatidylinositol 4 Kinase IIIß.

Journal of medicinal chemistry

Rutaganira FU, Fowler ML, McPhail JA, Gelman MA, Nguyen K, Xiong A, Dornan GL, Tavshanjian B, Glenn JS, Shokat KM, Burke JE

Voices of Chemical Biology: Charting the Next Decade.

Cell chemical biology

Kostic M, Crews CM, Hertweck C, Shokat K, Suga H

Using hydrogen deuterium exchange mass spectrometry to engineer optimized constructs for crystallization of protein complexes: Case study of PI4KIIIß with Rab11.

Protein science : a publication of the Protein Society

Fowler ML, McPhail JA, Jenkins ML, Masson GR, Rutaganira FU, Shokat KM, Williams RL, Burke JE

Cell Chemical Biology: Home of Exciting Chemical Biology.

Cell chemical biology

Kostic M, Crews CM, Hertweck C, Shokat K, Suga H

P-TEFb regulation of transcription termination factor Xrn2 revealed by a chemical genetic screen for Cdk9 substrates.

Genes & development

Sansó M, Levin RS, Lipp JJ, Wang VY, Greifenberg AK, Quezada EM, Ali A, Ghosh A, Larochelle S, Rana TM, Geyer M, Tong L, Shokat KM, Fisher RP

Analog sensitive chemical inhibition of the DEAD-box protein DDX3.

Protein science : a publication of the Protein Society

Floor SN, Barkovich KJ, Condon KJ, Shokat KM, Doudna JA

Inhibition of Calcium-Dependent Protein Kinase 1 (CDPK1) In Vitro by Pyrazolopyrimidine Derivatives Does Not Correlate with Sensitivity of Cryptosporidium parvum Growth in Cell Culture.

Antimicrobial agents and chemotherapy

Kuhlenschmidt TB, Rutaganira FU, Long S, Tang K, Shokat KM, Kuhlenschmidt MS, Sibley LD

Discovery and functional characterization of a neomorphic PTEN mutation.

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

Costa HA, Leitner MG, Sos ML, Mavrantoni A, Rychkova A, Johnson JR, Newton BW, Yee MC, De La Vega FM, Ford JM, Krogan NJ, Shokat KM, Oliver D, Halaszovich CR, Bustamante CD

Identification of AMPK Phosphorylation Sites Reveals a Network of Proteins Involved in Cell Invasion and Facilitates Large-Scale Substrate Prediction.

Cell metabolism

Schaffer BE, Levin RS, Hertz NT, Maures TJ, Schoof ML, Hollstein PE, Benayoun BA, Banko MR, Shaw RJ, Shokat KM, Brunet A

Small molecule inhibition of Csk alters affinity recognition by T cells.

eLife

Manz BN, Tan YX, Courtney AH, Rutaganira F, Palmer E, Shokat KM, Weiss A

SR protein kinases promote splicing of nonconsensus introns.

Nature structural & molecular biology

Lipp JJ, Marvin MC, Shokat KM, Guthrie C

WNK1-regulated inhibitory phosphorylation of the KCC2 cotransporter maintains the depolarizing action of GABA in immature neurons.

Science signaling

Friedel P, Kahle KT, Zhang J, Hertz N, Pisella LI, Buhler E, Schaller F, Duan J, Khanna AR, Bishop PN, Shokat KM, Medina I

Endoplasmic reticulum stress-independent activation of unfolded protein response kinases by a small molecule ATP-mimic.

eLife

Mendez AS, Alfaro J, Morales-Soto MA, Dar AC, McCullagh E, Gotthardt K, Li H, Acosta-Alvear D, Sidrauski C, Korennykh AV, Bernales S, Shokat KM, Walter P

Downregulation of MYCN through PI3K Inhibition in Mouse Models of Pediatric Neural Cancer.

Frontiers in oncology

Cage TA, Chanthery Y, Chesler L, Grimmer M, Knight Z, Shokat K, Weiss WA, Gustafson WC

Differential genetic interactions of yeast stress response MAPK pathways.

Molecular systems biology

Martin H, Shales M, Fernandez-Piñar P, Wei P, Molina M, Fiedler D, Shokat KM, Beltrao P, Lim W, Krogan NJ

The Tribbles 2 (TRB2) pseudokinase binds to ATP and autophosphorylates in a metal-independent manner.

The Biochemical journal

Bailey FP, Byrne DP, Oruganty K, Eyers CE, Novotny CJ, Shokat KM, Kannan N, Eyers PA

Overcoming myelosuppression due to synthetic lethal toxicity for FLT3-targeted acute myeloid leukemia therapy.

eLife

Warkentin AA, Lopez MS, Lasater EA, Lin K, He BL, Leung AY, Smith CC, Shah NP, Shokat KM

Radiotherapy followed by aurora kinase inhibition targets tumor-propagating cells in human glioblastoma.

Molecular cancer therapeutics

Li N, Maly DJ, Chanthery YH, Sirkis DW, Nakamura JL, Berger MS, James CD, Shokat KM, Weiss WA, Persson AI

Targeting osteosarcoma.

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

Reed DE, Shokat KM

Linking tumor mutations to drug responses via a quantitative chemical-genetic interaction map.

Cancer discovery

Martins MM, Zhou AY, Corella A, Horiuchi D, Yau C, Rakshandehroo T, Gordan JD, Levin RS, Johnson J, Jascur J, Shales M, Sorrentino A, Cheah J, Clemons PA, Shamji AF, Schreiber SL, Krogan NJ, Shokat KM, McCormick F, Goga A, Bandyopadhyay S

MST3 kinase phosphorylates TAO1/2 to enable Myosin Va function in promoting spine synapse development.

Neuron

Ultanir SK, Yadav S, Hertz NT, Oses-Prieto JA, Claxton S, Burlingame AL, Shokat KM, Jan LY, Jan YN

Reflecting on the past and looking forward to the future of bridging chemistry and biology.

Chemistry & biology

Crews C, Hertweck C, Shokat K, Suga H, Kostic M

Drugging MYCN through an allosteric transition in Aurora kinase A.

Cancer cell

Gustafson WC, Meyerowitz JG, Nekritz EA, Chen J, Benes C, Charron E, Simonds EF, Seeger R, Matthay KK, Hertz NT, Eilers M, Shokat KM, Weiss WA

TrkB kinase activity maintains synaptic function and structural integrity at adult neuromuscular junctions.

Journal of applied physiology (Bethesda, Md. : 1985)

Mantilla CB, Stowe JM, Sieck DC, Ermilov LG, Greising SM, Zhang C, Shokat KM, Sieck GC

Adipocyte ALK7 links nutrient overload to catecholamine resistance in obesity.

eLife

Guo T, Marmol P, Moliner A, Björnholm M, Zhang C, Shokat KM, Ibanez CF

A sharp T-cell antigen receptor signaling threshold for T-cell proliferation.

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

Au-Yeung BB, Zikherman J, Mueller JL, Ashouri JF, Matloubian M, Cheng DA, Chen Y, Shokat KM, Weiss A

Oncogene mimicry as a mechanism of primary resistance to BRAF inhibitors.

Cell reports

Sos ML, Levin RS, Gordan JD, Oses-Prieto JA, Webber JT, Salt M, Hann B, Burlingame AL, McCormick F, Bandyopadhyay S, Shokat KM

OCT1 is a high-capacity thiamine transporter that regulates hepatic steatosis and is a target of metformin.

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

Chen L, Shu Y, Liang X, Chen EC, Yee SW, Zur AA, Li S, Xu L, Keshari KR, Lin MJ, Chien HC, Zhang Y, Morrissey KM, Liu J, Ostrem J, Younger NS, Kurhanewicz J, Shokat KM, Ashrafi K, Giacomini KM

Quantitative and temporal requirements revealed for Zap70 catalytic activity during T cell development.

Nature immunology

Au-Yeung BB, Melichar HJ, Ross JO, Cheng DA, Zikherman J, Shokat KM, Robey EA, Weiss A

Structures of PI4KIIIß complexes show simultaneous recruitment of Rab11 and its effectors.

Science (New York, N.Y.)

Burke JE, Inglis AJ, Perisic O, Masson GR, McLaughlin SH, Rutaganira F, Shokat KM, Williams RL

Chemical genetics of rapamycin-insensitive TORC2 in S. cerevisiae.

Cell reports

Kliegman JI, Fiedler D, Ryan CJ, Xu YF, Su XY, Thomas D, Caccese MC, Cheng A, Shales M, Rabinowitz JD, Krogan NJ, Shokat KM

PLC-? and PI3K link cytokines to ERK activation in hematopoietic cells with normal and oncogenic Kras.

Science signaling

Diaz-Flores E, Goldschmidt H, Depeille P, Ng V, Akutagawa J, Krisman K, Crone M, Burgess MR, Williams O, Houseman B, Shokat K, Sampath D, Bollag G, Roose JP, Braun BS, Shannon K

Generation of a patient-derived chordoma xenograft and characterization of the phosphoproteome in a recurrent chordoma.

Journal of neurosurgery

Davies JM, Robinson AE, Cowdrey C, Mummaneni PV, Ducker GS, Shokat KM, Bollen A, Hann B, Phillips JJ

K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions.

Nature

Ostrem JM, Peters U, Sos ML, Wells JA, Shokat KM

Staurosporine-derived inhibitors broaden the scope of analog-sensitive kinase technology.

Journal of the American Chemical Society

Lopez MS, Choy JW, Peters U, Sos ML, Morgan DO, Shokat KM

EGFR phosphorylates tumor-derived EGFRvIII driving STAT3/5 and progression in glioblastoma.

Cancer cell

Fan QW, Cheng CK, Gustafson WC, Charron E, Zipper P, Wong RA, Chen J, Lau J, Knobbe-Thomsen C, Weller M, Jura N, Reifenberger G, Shokat KM, Weiss WA

A neo-substrate that amplifies catalytic activity of parkinson's-disease-related kinase PINK1.

Cell

Hertz NT, Berthet A, Sos ML, Thorn KS, Burlingame AL, Nakamura K, Shokat KM

Structure-guided inhibitor design expands the scope of analog-sensitive kinase technology.

ACS chemical biology

Zhang C, Lopez MS, Dar AC, Ladow E, Finkbeiner S, Yun CH, Eck MJ, Shokat KM

Myc and mTOR converge on a common node in protein synthesis control that confers synthetic lethality in Myc-driven cancers.

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

Pourdehnad M, Truitt ML, Siddiqi IN, Ducker GS, Shokat KM, Ruggero D

PTEN expression is consistent in colorectal cancer primaries and metastases and associates with patient survival.

Cancer medicine

Atreya CE, Sangale Z, Xu N, Matli MR, Tikishvili E, Welbourn W, Stone S, Shokat KM, Warren RS

A Cdk7-Cdk4 T-loop phosphorylation cascade promotes G1 progression.

Molecular cell

Schachter MM, Merrick KA, Larochelle S, Hirschi A, Zhang C, Shokat KM, Rubin SM, Fisher RP

Optimizing small molecule inhibitors of calcium-dependent protein kinase 1 to prevent infection by Toxoplasma gondii.

Journal of medicinal chemistry

Lourido S, Zhang C, Lopez MS, Tang K, Barks J, Wang Q, Wildman SA, Shokat KM, Sibley LD

Glucose sensor O-GlcNAcylation coordinates with phosphorylation to regulate circadian clock.

Cell metabolism

Kaasik K, Kivimäe S, Allen JJ, Chalkley RJ, Huang Y, Baer K, Kissel H, Burlingame AL, Shokat KM, Ptácek LJ, Fu YH

News from the Chemistry & Biology editorial team.

Chemistry & biology

Crews C, Shokat K, Suga H, Kostic M

A chemical genetic approach reveals distinct EphB signaling mechanisms during brain development.

Nature neuroscience

Soskis MJ, Ho HY, Bloodgood BL, Robichaux MA, Malik AN, Ataman B, Rubin AA, Zieg J, Zhang C, Shokat KM, Sharma N, Cowan CW, Greenberg ME

Cyclin-dependent kinase control of the initiation-to-elongation switch of RNA polymerase II.

Nature structural & molecular biology

Larochelle S, Amat R, Glover-Cutter K, Sansó M, Zhang C, Allen JJ, Shokat KM, Bentley DL, Fisher RP

Chemical genetics reveals a specific requirement for Cdk2 activity in the DNA damage response and identifies Nbs1 as a Cdk2 substrate in human cells.

PLoS genetics

Wohlbold L, Merrick KA, De S, Amat R, Kim JH, Larochelle S, Allen JJ, Zhang C, Shokat KM, Petrini JH, Fisher RP

A positive feedback loop links opposing functions of P-TEFb/Cdk9 and histone H2B ubiquitylation to regulate transcript elongation in fission yeast.

PLoS genetics

Sansó M, Lee KM, Viladevall L, Jacques PÉ, Pagé V, Nagy S, Racine A, St Amour CV, Zhang C, Shokat KM, Schwer B, Robert F, Fisher RP, Tanny JC

Dual blockade of lipid and cyclin-dependent kinases induces synthetic lethality in malignant glioma.

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

Cheng CK, Gustafson WC, Charron E, Houseman BT, Zunder E, Goga A, Gray NS, Pollok B, Oakes SA, James CD, Shokat KM, Weiss WA, Fan QW

Integrin a9ß1 in airway smooth muscle suppresses exaggerated airway narrowing.

The Journal of clinical investigation

Chen C, Kudo M, Rutaganira F, Takano H, Lee C, Atakilit A, Robinett KS, Uede T, Wolters PJ, Shokat KM, Huang X, Sheppard D

In vivo conditions to identify Prkci phosphorylation targets using the analog-sensitive kinase method in zebrafish.

PloS one

Cibrián Uhalte E, Kirchner M, Hellwig N, Allen JJ, Donat S, Shokat KM, Selbach M, Abdelilah-Seyfried S

Carbonyl reductase 1 offers a novel therapeutic target to enhance leukemia treatment by arsenic trioxide.

Cancer research

Jang M, Kim Y, Won H, Lim S, K R J, Dashdorj A, Min YH, Kim SY, Shokat KM, Ha J, Kim SS

Hierarchical modularity and the evolution of genetic interactomes across species.

Molecular cell

Ryan CJ, Roguev A, Patrick K, Xu J, Jahari H, Tong Z, Beltrao P, Shales M, Qu H, Collins SR, Kliegman JI, Jiang L, Kuo D, Tosti E, Kim HS, Edelmann W, Keogh MC, Greene D, Tang C, Cunningham P, Shokat KM, Cagney G, Svensson JP, Guthrie C, Espenshade PJ, Ideker T, Krogan NJ

Orm protein phosphoregulation mediates transient sphingolipid biosynthesis response to heat stress via the Pkh-Ypk and Cdc55-PP2A pathways.

Molecular biology of the cell

Sun Y, Miao Y, Yamane Y, Zhang C, Shokat KM, Takematsu H, Kozutsumi Y, Drubin DG

Separate domains of fission yeast Cdk9 (P-TEFb) are required for capping enzyme recruitment and primed (Ser7-phosphorylated) Rpb1 carboxyl-terminal domain substrate recognition.

Molecular and cellular biology

St Amour CV, Sansó M, Bösken CA, Lee KM, Larochelle S, Zhang C, Shokat KM, Geyer M, Fisher RP

Chemical-genetic analysis of cyclin dependent kinase 2 function reveals an important role in cellular transformation by multiple oncogenic pathways.

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

Horiuchi D, Huskey NE, Kusdra L, Wohlbold L, Merrick KA, Zhang C, Creasman KJ, Shokat KM, Fisher RP, Goga A

Kinetics of inhibitor cycling underlie therapeutic disparities between EGFR-driven lung and brain cancers.

Cancer discovery

Barkovich KJ, Hariono S, Garske AL, Zhang J, Blair JA, Fan QW, Shokat KM, Nicolaides T, Weiss WA

Chemical genetic identification of NDR1/2 kinase substrates AAK1 and Rabin8 Uncovers their roles in dendrite arborization and spine development.

Neuron

Ultanir SK, Hertz NT, Li G, Ge WP, Burlingame AL, Pleasure SJ, Shokat KM, Jan LY, Jan YN

The translational landscape of mTOR signalling steers cancer initiation and metastasis.

Nature

Hsieh AC, Liu Y, Edlind MP, Ingolia NT, Janes MR, Sher A, Shi EY, Stumpf CR, Christensen C, Bonham MJ, Wang S, Ren P, Martin M, Jessen K, Feldman ME, Weissman JS, Shokat KM, Rommel C, Ruggero D

Combination of ATP-competitive mammalian target of rapamycin inhibitors with standard chemotherapy for colorectal cancer.

Investigational new drugs

Atreya CE, Ducker GS, Feldman ME, Bergsland EK, Warren RS, Shokat KM

Development of a chemical genetic approach for human aurora B kinase identifies novel substrates of the chromosomal passenger complex.

Molecular & cellular proteomics : MCP

Hengeveld RC, Hertz NT, Vromans MJ, Zhang C, Burlingame AL, Shokat KM, Lens SM

Covalent cross-linking of kinases with their corresponding peptide substrates.

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

Statsuk AV, Shokat KM

Chemical genetic screen for AMPKa2 substrates uncovers a network of proteins involved in mitosis.

Molecular cell

Banko MR, Allen JJ, Schaffer BE, Wilker EW, Tsou P, White JL, Villén J, Wang B, Kim SR, Sakamoto K, Gygi SP, Cantley LC, Yaffe MB, Shokat KM, Brunet A

Generation of a set of conditional analog-sensitive alleles of essential protein kinases in the fission yeast Schizosaccharomyces pombe.

Cell cycle (Georgetown, Tex.)

Cipak L, Zhang C, Kovacikova I, Rumpf C, Miadokova E, Shokat KM, Gregan J

Genetic deletion of trkB.T1 increases neuromuscular function.

American journal of physiology. Cell physiology

Dorsey SG, Lovering RM, Renn CL, Leitch CC, Liu X, Tallon LJ, Sadzewicz LD, Pratap A, Ott S, Sengamalay N, Jones KM, Barrick C, Fulgenzi G, Becker J, Voelker K, Talmadge R, Harvey BK, Wyatt RM, Vernon-Pitts E, Zhang C, Shokat K, Fraser-Liggett C, Balice-Gordon RJ, Tessarollo L, Ward CW

The Cryptosporidium parvum kinome.

BMC genomics

Artz JD, Wernimont AK, Allali-Hassani A, Zhao Y, Amani M, Lin YH, Senisterra G, Wasney GA, Fedorov O, King O, Roos A, Lunin VV, Qiu W, Finerty P, Hutchinson A, Chau I, von Delft F, MacKenzie F, Lew J, Kozieradzki I, Vedadi M, Schapira M, Zhang C, Shokat K, Heightman T, Hui R

Feedback circuits monitor and adjust basal Lck-dependent events in T cell receptor signaling.

Science signaling

Schoenborn JR, Tan YX, Zhang C, Shokat KM, Weiss A

The mammalian target of rapamycin regulates cholesterol biosynthetic gene expression and exhibits a rapamycin-resistant transcriptional profile.

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

Wang BT, Ducker GS, Barczak AJ, Barbeau R, Erle DJ, Shokat KM

Chemical genetic strategy for targeting protein kinases based on covalent complementarity.

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

Garske AL, Peters U, Cortesi AT, Perez JL, Shokat KM

TrkB and protein kinase M? regulate synaptic localization of PSD-95 in developing cortex.

The Journal of neuroscience : the official journal of the Society for Neuroscience

Yoshii A, Murata Y, Kim J, Zhang C, Shokat KM, Constantine-Paton M

Cofactor-mediated conformational control in the bifunctional kinase/RNase Ire1.

BMC biology

Korennykh AV, Egea PF, Korostelev AA, Finer-Moore J, Stroud RM, Zhang C, Shokat KM, Walter P

Structural and functional basis for RNA cleavage by Ire1.

BMC biology

Korennykh AV, Korostelev AA, Egea PF, Finer-Moore J, Stroud RM, Zhang C, Shokat KM, Walter P

Autophagy suppression promotes apoptotic cell death in response to inhibition of the PI3K-mTOR pathway in pancreatic adenocarcinoma.

Journal of molecular medicine (Berlin, Germany)

Mirzoeva OK, Hann B, Hom YK, Debnath J, Aftab D, Shokat K, Korn WM

Switching Cdk2 on or off with small molecules to reveal requirements in human cell proliferation.

Molecular cell

Merrick KA, Wohlbold L, Zhang C, Allen JJ, Horiuchi D, Huskey NE, Goga A, Shokat KM, Fisher RP

A Raf-induced allosteric transition of KSR stimulates phosphorylation of MEK.

Nature

Brennan DF, Dar AC, Hertz NT, Chao WC, Burlingame AL, Shokat KM, Barford D

Chemistry & Biology editors announce changes to the editorial team.

Chemistry & biology

Crews C, Shokat K, Wohlleben W, Kostic M

Dose-dependent effects of focal fractionated irradiation on secondary malignant neoplasms in Nf1 mutant mice.

Cancer research

Nakamura JL, Phong C, Pinarbasi E, Kogan SC, Vandenberg S, Horvai AE, Faddegon BA, Fiedler D, Shokat K, Houseman BT, Chao R, Pieper RO, Shannon K

Sensitizing plant protein kinases to specific inhibition by ATP-competitive molecules.

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

Salomon D, Zhang C, Shokat KM, Sessa G

Phosphoproteomic analysis reveals interconnected system-wide responses to perturbations of kinases and phosphatases in yeast.

Science signaling

Bodenmiller B, Wanka S, Kraft C, Urban J, Campbell D, Pedrioli PG, Gerrits B, Picotti P, Lam H, Vitek O, Brusniak MY, Roschitzki B, Zhang C, Shokat KM, Schlapbach R, Colman-Lerner A, Nolan GP, Nesvizhskii AI, Peter M, Loewith R, von Mering C, Aebersold R

Rewiring of genetic networks in response to DNA damage.

Science (New York, N.Y.)

Bandyopadhyay S, Mehta M, Kuo D, Sung MK, Chuang R, Jaehnig EJ, Bodenmiller B, Licon K, Copeland W, Shales M, Fiedler D, Dutkowski J, Guénolé A, van Attikum H, Shokat KM, Kolodner RD, Huh WK, Aebersold R, Keogh MC, Krogan NJ, Ideker T

Constitutive mTORC1 activation by a herpesvirus Akt surrogate stimulates mRNA translation and viral replication.

Genes & development

Chuluunbaatar U, Roller R, Feldman ME, Brown S, Shokat KM, Mohr I

Akt and autophagy cooperate to promote survival of drug-resistant glioma.

Science signaling

Fan QW, Cheng C, Hackett C, Feldman M, Houseman BT, Nicolaides T, Haas-Kogan D, James CD, Oakes SA, Debnath J, Shokat KM, Weiss WA

A genetically selective inhibitor demonstrates a function for the kinase Zap70 in regulatory T cells independent of its catalytic activity.

Nature immunology

Au-Yeung BB, Levin SE, Zhang C, Hsu LY, Cheng DA, Killeen N, Shokat KM, Weiss A

A kinase cascade leading to Rab11-FIP5 controls transcytosis of the polymeric immunoglobulin receptor.

Nature cell biology

Su T, Bryant DM, Luton F, Vergés M, Ulrich SM, Hansen KC, Datta A, Eastburn DJ, Burlingame AL, Shokat KM, Mostov KE

GABAA receptor trafficking is regulated by protein kinase C(epsilon) and the N-ethylmaleimide-sensitive factor.

The Journal of neuroscience : the official journal of the Society for Neuroscience

Chou WH, Wang D, McMahon T, Qi ZH, Song M, Zhang C, Shokat KM, Messing RO

Human carbonyl reductase 1 upregulated by hypoxia renders resistance to apoptosis in hepatocellular carcinoma cells.

Journal of hepatology

Tak E, Lee S, Lee J, Rashid MA, Kim YW, Park JH, Park WS, Shokat KM, Ha J, Kim SS

Chemical-genomic dissection of the CTD code.

Nature structural & molecular biology

Tietjen JR, Zhang DW, Rodríguez-Molina JB, White BE, Akhtar MS, Heidemann M, Li X, Chapman RD, Shokat K, Keles S, Eick D, Ansari AZ

Mps1 directs the assembly of Cdc20 inhibitory complexes during interphase and mitosis to control M phase timing and spindle checkpoint signaling.

The Journal of cell biology

Maciejowski J, George KA, Terret ME, Zhang C, Shokat KM, Jallepalli PV

Synthesis and evaluation of indazole based analog sensitive Akt inhibitors.

Molecular bioSystems

Okuzumi T, Ducker GS, Zhang C, Aizenstein B, Hoffman R, Shokat KM

Calcium-dependent protein kinase 1 is an essential regulator of exocytosis in Toxoplasma.

Nature

Lourido S, Shuman J, Zhang C, Shokat KM, Hui R, Sibley LD

Shaping development of autophagy inhibitors with the structure of the lipid kinase Vps34.

Science (New York, N.Y.)

Miller S, Tavshanjian B, Oleksy A, Perisic O, Houseman BT, Shokat KM, Williams RL

mTOR complex-2 activates ENaC by phosphorylating SGK1.

Journal of the American Society of Nephrology : JASN

Lu M, Wang J, Jones KT, Ives HE, Feldman ME, Yao LJ, Shokat KM, Ashrafi K, Pearce D

RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF.

Nature

Poulikakos PI, Zhang C, Bollag G, Shokat KM, Rosen N

Genetic dissection of the oncogenic mTOR pathway reveals druggable addiction to translational control via 4EBP-eIF4E.

Cancer cell

Hsieh AC, Costa M, Zollo O, Davis C, Feldman ME, Testa JR, Meyuhas O, Shokat KM, Ruggero D

Chemical genetic approach for kinase-substrate mapping by covalent capture of thiophosphopeptides and analysis by mass spectrometry.

Current protocols in chemical biology

Hertz NT, Wang BT, Allen JJ, Zhang C, Dar AC, Burlingame AL, Shokat KM

Mutant Ikzf1, KrasG12D, and Notch1 cooperate in T lineage leukemogenesis and modulate responses to targeted agents.

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

Dail M, Li Q, McDaniel A, Wong J, Akagi K, Huang B, Kang HC, Kogan SC, Shokat K, Wolff L, Braun BS, Shannon K

The p110delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors.

Nature chemical biology

Berndt A, Miller S, Williams O, Le DD, Houseman BT, Pacold JI, Gorrec F, Hon WC, Liu Y, Rommel C, Gaillard P, Rückle T, Schwarz MK, Shokat KM, Shaw JP, Williams RL

Discovery of dual inhibitors of the immune cell PI3Ks p110delta and p110gamma: a prototype for new anti-inflammatory drugs.

Chemistry & biology

Williams O, Houseman BT, Kunkel EJ, Aizenstein B, Hoffman R, Knight ZA, Shokat KM

Dynamic regulation of a metabolic multi-enzyme complex by protein kinase CK2.

The Journal of biological chemistry

An S, Kyoung M, Allen JJ, Shokat KM, Benkovic SJ

Targeting the cancer kinome through polypharmacology.

Nature reviews. Cancer

Knight ZA, Lin H, Shokat KM

The p110 delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors.

Nature chemical biology

Berndt A, Miller S, Williams O, Le DD, Houseman BT, Pacold JI, Gorrec F, Hon WC, Liu Y, Rommel C, Gaillard P, Rückle T, Schwarz MK, Shokat KM, Shaw JP, Williams RL

Resiliency and vulnerability in the HER2-HER3 tumorigenic driver.

Science translational medicine

Amin DN, Sergina N, Ahuja D, McMahon M, Blair JA, Wang D, Hann B, Koch KM, Shokat KM, Moasser MM

Transforming growth factor beta1 inhibits cystic fibrosis transmembrane conductance regulator-dependent cAMP-stimulated alveolar epithelial fluid transport via a phosphatidylinositol 3-kinase-dependent mechanism.

The Journal of biological chemistry

Roux J, Carles M, Koh H, Goolaerts A, Ganter MT, Chesebro BB, Howard M, Houseman BT, Finkbeiner W, Shokat KM, Paquet AC, Matthay MA, Pittet JF

Regulation of meiotic recombination via Mek1-mediated Rad54 phosphorylation.

Molecular cell

Niu H, Wan L, Busygina V, Kwon Y, Allen JA, Li X, Kunz RC, Kubota K, Wang B, Sung P, Shokat KM, Gygi SP, Hollingsworth NM

Arterial-venous segregation by selective cell sprouting: an alternative mode of blood vessel formation.

Science (New York, N.Y.)

Herbert SP, Huisken J, Kim TN, Feldman ME, Houseman BT, Wang RA, Shokat KM, Stainier DY

Use of a semisynthetic epitope to probe histidine kinase activity and regulation.

Analytical biochemistry

Carlson HK, Plate L, Price MS, Allen JJ, Shokat KM, Marletta MA

Identifying genotype-dependent efficacy of single and combined PI3K- and MAPK-pathway inhibition in cancer.

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

Sos ML, Fischer S, Ullrich R, Peifer M, Heuckmann JM, Koker M, Heynck S, Stückrath I, Weiss J, Fischer F, Michel K, Goel A, Regales L, Politi KA, Perera S, Getlik M, Heukamp LC, Ansén S, Zander T, Beroukhim R, Kashkar H, Shokat KM, Sellers WR, Rauh D, Orr C, Hoeflich KP, Friedman L, Wong KK, Pao W, Thomas RK

TFIIH-associated Cdk7 kinase functions in phosphorylation of C-terminal domain Ser7 residues, promoter-proximal pausing, and termination by RNA polymerase II.

Molecular and cellular biology

Glover-Cutter K, Larochelle S, Erickson B, Zhang C, Shokat K, Fisher RP, Bentley DL

Phosphorylation of the transcription elongation factor Spt5 by yeast Bur1 kinase stimulates recruitment of the PAF complex.

Molecular and cellular biology

Liu Y, Warfield L, Zhang C, Luo J, Allen J, Lang WH, Ranish J, Shokat KM, Hahn S

PIKfyve regulation of endosome-linked pathways.

Traffic (Copenhagen, Denmark)

de Lartigue J, Polson H, Feldman M, Shokat K, Tooze SA, Urbé S, Clague MJ

Evolution of phosphoregulation: comparison of phosphorylation patterns across yeast species.

PLoS biology

Beltrao P, Trinidad JC, Fiedler D, Roguev A, Lim WA, Shokat KM, Burlingame AL, Krogan NJ

Inhibitor hijacking of Akt activation.

Nature chemical biology

Okuzumi T, Fiedler D, Zhang C, Gray DC, Aizenstein B, Hoffman R, Shokat KM

Plk1 self-organization and priming phosphorylation of HsCYK-4 at the spindle midzone regulate the onset of division in human cells.

PLoS biology

Burkard ME, Maciejowski J, Rodriguez-Bravo V, Repka M, Lowery DM, Clauser KR, Zhang C, Shokat KM, Carr SA, Yaffe MB, Jallepalli PV

Tuning the activation threshold of a kinase network by nested feedback loops.

Science (New York, N.Y.)

Justman QA, Serber Z, Ferrell JE, El-Samad H, Shokat KM

Bypassing kinase activity of the tomato Pto resistance protein with small molecule ligands.

The Journal of biological chemistry

Salomon D, Bonshtien A, Mayrose M, Zhang C, Shokat KM, Sessa G

TFIIH and P-TEFb coordinate transcription with capping enzyme recruitment at specific genes in fission yeast.

Molecular cell

Viladevall L, St Amour CV, Rosebrock A, Schneider S, Zhang C, Allen JJ, Shokat KM, Schwer B, Leatherwood JK, Fisher RP

Phosphorylation of the SRC epithelial substrate Trask is tightly regulated in normal epithelia but widespread in many human epithelial cancers.

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

Wong CH, Baehner FL, Spassov DS, Ahuja D, Wang D, Hann B, Blair J, Shokat K, Welm AL, Moasser MM

Functional organization of the S. cerevisiae phosphorylation network.

Cell

Fiedler D, Braberg H, Mehta M, Chechik G, Cagney G, Mukherjee P, Silva AC, Shales M, Collins SR, van Wageningen S, Kemmeren P, Holstege FC, Weissman JS, Keogh MC, Koller D, Shokat KM, Krogan NJ

Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2.

PLoS biology

Feldman ME, Apsel B, Uotila A, Loewith R, Knight ZA, Ruggero D, Shokat KM

A complex-based reconstruction of the Saccharomyces cerevisiae interactome.

Molecular & cellular proteomics : MCP

Wang H, Kakaradov B, Collins SR, Karotki L, Fiedler D, Shales M, Shokat KM, Walther TC, Krogan NJ, Koller D

EGFR signals to mTOR through PKC and independently of Akt in glioma.

Science signaling

Fan QW, Cheng C, Knight ZA, Haas-Kogan D, Stokoe D, James CD, McCormick F, Shokat KM, Weiss WA

Basal subtype and MAPK/ERK kinase (MEK)-phosphoinositide 3-kinase feedback signaling determine susceptibility of breast cancer cells to MEK inhibition.

Cancer research

Mirzoeva OK, Das D, Heiser LM, Bhattacharya S, Siwak D, Gendelman R, Bayani N, Wang NJ, Neve RM, Guan Y, Hu Z, Knight Z, Feiler HS, Gascard P, Parvin B, Spellman PT, Shokat KM, Wyrobek AJ, Bissell MJ, McCormick F, Kuo WL, Mills GB, Gray JW, Korn WM

Generation of a novel system for studying spleen tyrosine kinase function in macrophages and B cells.

Journal of immunology (Baltimore, Md. : 1950)

Miller AL, Zhang C, Shokat KM, Lowell CA

SHIP prevents lipopolysaccharide from triggering an antiviral response in mice.

Blood

Sly LM, Hamilton MJ, Kuroda E, Ho VW, Antignano FL, Omeis SL, van Netten-Thomas CJ, Wong D, Brugger HK, Williams O, Feldman ME, Houseman BT, Fiedler D, Shokat KM, Krystal G

Cdk1-dependent phosphorylation of Cdc13 coordinates telomere elongation during cell-cycle progression.

Cell

Li S, Makovets S, Matsuguchi T, Blethrow JD, Shokat KM, Blackburn EH

Tuning a three-component reaction for trapping kinase substrate complexes.

Journal of the American Chemical Society

Statsuk AV, Maly DJ, Seeliger MA, Fabian MA, Biggs WH, Lockhart DJ, Zarrinkar PP, Kuriyan J, Shokat KM

The unfolded protein response signals through high-order assembly of Ire1.

Nature

Korennykh AV, Egea PF, Korostelev AA, Finer-Moore J, Zhang C, Shokat KM, Stroud RM, Walter P

Tissue-specific PKA inhibition using a chemical genetic approach and its application to studies on sperm capacitation.

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

Morgan DJ, Weisenhaus M, Shum S, Su T, Zheng R, Zhang C, Shokat KM, Hille B, Babcock DF, McKnight GS

Distinct activation pathways confer cyclin-binding specificity on Cdk1 and Cdk2 in human cells.

Molecular cell

Merrick KA, Larochelle S, Zhang C, Allen JJ, Shokat KM, Fisher RP

Distinct roles of class IA PI3K isoforms in primary and immortalised macrophages.

Journal of cell science

Papakonstanti EA, Zwaenepoel O, Bilancio A, Burns E, Nock GE, Houseman B, Shokat K, Ridley AJ, Vanhaesebroeck B

Protein kinase Cdelta regulates ethanol intoxication and enhancement of GABA-stimulated tonic current.

The Journal of neuroscience : the official journal of the Society for Neuroscience

Choi DS, Wei W, Deitchman JK, Kharazia VN, Lesscher HM, McMahon T, Wang D, Qi ZH, Sieghart W, Zhang C, Shokat KM, Mody I, Messing RO

Structure and substrate recruitment of the human spindle checkpoint kinase Bub1.

Molecular cell

Kang J, Yang M, Li B, Qi W, Zhang C, Shokat KM, Tomchick DR, Machius M, Yu H

A chemical genomics study identifies Snf1 as a repressor of GCN4 translation.

The Journal of biological chemistry

Shirra MK, McCartney RR, Zhang C, Shokat KM, Schmidt MC, Arndt KM

Dual inhibition of PI3Kalpha and mTOR as an alternative treatment for Kaposi's sarcoma.

Cancer research

Chaisuparat R, Hu J, Jham BC, Knight ZA, Shokat KM, Montaner S

Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.

Nature chemical biology

Apsel B, Blair JA, Gonzalez B, Nazif TM, Feldman ME, Aizenstein B, Hoffman R, Williams RL, Shokat KM, Knight ZA

The yeast LATS/Ndr kinase Cbk1 regulates growth via Golgi-dependent glycosylation and secretion.

Molecular biology of the cell

Kurischko C, Kuravi VK, Wannissorn N, Nazarov PA, Husain M, Zhang C, Shokat KM, McCaffery JM, Luca FC

A chemical screen in diverse breast cancer cell lines reveals genetic enhancers and suppressors of sensitivity to PI3K isoform-selective inhibition.

The Biochemical journal

Torbett NE, Luna-Moran A, Knight ZA, Houk A, Moasser M, Weiss W, Shokat KM, Stokoe D

Genetic or pharmaceutical blockade of p110delta phosphoinositide 3-kinase enhances IgE production.

The Journal of allergy and clinical immunology

Zhang TT, Okkenhaug K, Nashed BF, Puri KD, Knight ZA, Shokat KM, Vanhaesebroeck B, Marshall AJ

PIK3CA cooperates with other phosphatidylinositol 3'-kinase pathway mutations to effect oncogenic transformation.

Cancer research

Oda K, Okada J, Timmerman L, Rodriguez-Viciana P, Stokoe D, Shoji K, Taketani Y, Kuramoto H, Knight ZA, Shokat KM, McCormick F

Human carbonyl reductase 1 is an S-nitrosoglutathione reductase.

The Journal of biological chemistry

Bateman RL, Rauh D, Tavshanjian B, Shokat KM

The effect of H3K79 dimethylation and H4K20 trimethylation on nucleosome and chromatin structure.

Nature structural & molecular biology

Lu X, Simon MD, Chodaparambil JV, Hansen JC, Shokat KM, Luger K

Ablation of PI3K blocks BCR-ABL leukemogenesis in mice, and a dual PI3K/mTOR inhibitor prevents expansion of human BCR-ABL+ leukemia cells.

The Journal of clinical investigation

Kharas MG, Janes MR, Scarfone VM, Lilly MB, Knight ZA, Shokat KM, Fruman DA

Discovery of drug-resistant and drug-sensitizing mutations in the oncogenic PI3K isoform p110 alpha.

Cancer cell

Zunder ER, Knight ZA, Houseman BT, Apsel B, Shokat KM

The brain-derived neurotrophic factor receptor TrkB is critical for the acquisition but not expression of conditioned incentive value.

The European journal of neuroscience

Johnson AW, Chen X, Crombag HS, Zhang C, Smith DR, Shokat KM, Gallagher M, Holland PC, Ginty DD

Activity of the p110-alpha subunit of phosphatidylinositol-3-kinase is required for activation of epithelial sodium transport.

American journal of physiology. Renal physiology

Wang J, Knight ZA, Fiedler D, Williams O, Shokat KM, Pearce D

An integrated platform of genomic assays reveals small-molecule bioactivities.

Nature chemical biology

Hoon S, Smith AM, Wallace IM, Suresh S, Miranda M, Fung E, Proctor M, Shokat KM, Zhang C, Davis RW, Giaever G, St Onge RP, StOnge RP, Nislow C

Nuclear HuR accumulation through phosphorylation by Cdk1.

Genes & development

Kim HH, Abdelmohsen K, Lal A, Pullmann R, Yang X, Galban S, Srikantan S, Martindale JL, Blethrow J, Shokat KM, Gorospe M

T cell receptor signaling controls Foxp3 expression via PI3K, Akt, and mTOR.

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

Sauer S, Bruno L, Hertweck A, Finlay D, Leleu M, Spivakov M, Knight ZA, Cobb BS, Cantrell D, O'Connor E, Shokat KM, Fisher AG, Merkenschlager M

Analysis of 3-phosphoinositide-dependent kinase-1 signaling and function in ES cells.

Experimental cell research

Tamgüney T, Zhang C, Fiedler D, Shokat K, Stokoe D

Characterization of structurally distinct, isoform-selective phosphoinositide 3'-kinase inhibitors in combination with radiation in the treatment of glioblastoma.

Molecular cancer therapeutics

Chen JS, Zhou LJ, Entin-Meer M, Yang X, Donker M, Knight ZA, Weiss W, Shokat KM, Haas-Kogan D, Stokoe D

Inhibition of ZAP-70 kinase activity via an analog-sensitive allele blocks T cell receptor and CD28 superagonist signaling.

The Journal of biological chemistry

Levin SE, Zhang C, Kadlecek TA, Shokat KM, Weiss A

Cdc28-Clb5 (CDK-S) and Cdc7-Dbf4 (DDK) collaborate to initiate meiotic recombination in yeast.

Genes & development

Wan L, Niu H, Futcher B, Zhang C, Shokat KM, Boulton SJ, Hollingsworth NM

Covalent capture of kinase-specific phosphopeptides reveals Cdk1-cyclin B substrates.

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

Blethrow JD, Glavy JS, Morgan DO, Shokat KM

Design of drug-resistant alleles of type-III phosphatidylinositol 4-kinases using mutagenesis and molecular modeling.

Biochemistry

Balla A, Tuymetova G, Toth B, Szentpetery Z, Zhao X, Knight ZA, Shokat K, Steinbach PJ, Balla T

Maintenance of hormone-sensitive phosphoinositide pools in the plasma membrane requires phosphatidylinositol 4-kinase IIIalpha.

Molecular biology of the cell

Balla A, Kim YJ, Varnai P, Szentpetery Z, Knight Z, Shokat KM, Balla T

Recognizing and exploiting differences between RNAi and small-molecule inhibitors.

Nature chemical biology

Weiss WA, Taylor SS, Shokat KM

IRE1 signaling affects cell fate during the unfolded protein response.

Science (New York, N.Y.)

Lin JH, Li H, Yasumura D, Cohen HR, Zhang C, Panning B, Shokat KM, Lavail MM, Walter P

Access denied: Snf1 activation loop phosphorylation is controlled by availability of the phosphorylated threonine 210 to the PP1 phosphatase.

The Journal of biological chemistry

Rubenstein EM, McCartney RR, Zhang C, Shokat KM, Shirra MK, Arndt KM, Schmidt MC

A coupled chemical-genetic and bioinformatic approach to Polo-like kinase pathway exploration.

Chemistry & biology

Snead JL, Sullivan M, Lowery DM, Cohen MS, Zhang C, Randle DH, Taunton J, Yaffe MB, Morgan DO, Shokat KM

A surface on the androgen receptor that allosterically regulates coactivator binding.

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

Estébanez-Perpiñá E, Arnold LA, Arnold AA, Nguyen P, Rodrigues ED, Mar E, Bateman R, Pallai P, Shokat KM, Baxter JD, Guy RK, Webb P, Fletterick RJ

Suppression of p53-dependent senescence by the JNK signal transduction pathway.

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

Das M, Jiang F, Sluss HK, Zhang C, Shokat KM, Flavell RA, Davis RJ

Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2 subunits.

The Journal of biological chemistry

Qi ZH, Song M, Wallace MJ, Wang D, Newton PM, McMahon T, Chou WH, Zhang C, Shokat KM, Messing RO

A remodelled protease that cleaves phosphotyrosine substrates.

Journal of the American Chemical Society

Knight ZA, Garrison JL, Chan K, King DS, Shokat KM

A dual phosphoinositide-3-kinase alpha/mTOR inhibitor cooperates with blockade of epidermal growth factor receptor in PTEN-mutant glioma.

Cancer research

Fan QW, Cheng CK, Nicolaides TP, Hackett CS, Knight ZA, Shokat KM, Weiss WA

Glutathione traps formaldehyde by formation of a bicyclo[4.4.1]undecane adduct.

Organic & biomolecular chemistry

Bateman R, Rauh D, Shokat KM

A semisynthetic epitope for kinase substrates.

Nature methods

Allen JJ, Li M, Brinkworth CS, Paulson JL, Wang D, Hübner A, Chou WH, Davis RJ, Burlingame AL, Messing RO, Katayama CD, Hedrick SM, Shokat KM

HIV-1 Nef assembles a Src family kinase-ZAP-70/Syk-PI3K cascade to downregulate cell-surface MHC-I.

Cell host & microbe

Hung CH, Thomas L, Ruby CE, Atkins KM, Morris NP, Knight ZA, Scholz I, Barklis E, Weinberg AD, Shokat KM, Thomas G

Chemical inhibition of the TFIIH-associated kinase Cdk7/Kin28 does not impair global mRNA synthesis.

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

Kanin EI, Kipp RT, Kung C, Slattery M, Viale A, Hahn S, Shokat KM, Ansari AZ

Requirements for Cdk7 in the assembly of Cdk1/cyclin B and activation of Cdk2 revealed by chemical genetics in human cells.

Molecular cell

Larochelle S, Merrick KA, Terret ME, Wohlbold L, Barboza NM, Zhang C, Shokat KM, Jallepalli PV, Fisher RP

The site-specific installation of methyl-lysine analogs into recombinant histones.

Cell

Simon MD, Chu F, Racki LR, de la Cruz CC, Burlingame AL, Panning B, Narlikar GJ, Shokat KM

Chemical genetics reveals the requirement for Polo-like kinase 1 activity in positioning RhoA and triggering cytokinesis in human cells.

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

Burkard ME, Randall CL, Larochelle S, Zhang C, Shokat KM, Fisher RP, Jallepalli PV

Structure-guided development of affinity probes for tyrosine kinases using chemical genetics.

Nature chemical biology

Blair JA, Rauh D, Kung C, Yun CH, Fan QW, Rode H, Zhang C, Eck MJ, Weiss WA, Shokat KM

Escape from HER-family tyrosine kinase inhibitor therapy by the kinase-inactive HER3.

Nature

Sergina NV, Rausch M, Wang D, Blair J, Hann B, Shokat KM, Moasser MM

A membrane capture assay for lipid kinase activity.

Nature protocols

Knight ZA, Feldman ME, Balla A, Balla T, Shokat KM

Construction of conditional analog-sensitive kinase alleles in the fission yeast Schizosaccharomyces pombe.

Nature protocols

Gregan J, Zhang C, Rumpf C, Cipak L, Li Z, Uluocak P, Nasmyth K, Shokat KM

Structure and properties of a re-engineered homeodomain protein-DNA interface.

ACS chemical biology

Simon MD, Feldman ME, Rauh D, Maris AE, Wemmer DE, Shokat KM

Phosphatidylinositol 4-kinase IIIbeta regulates the transport of ceramide between the endoplasmic reticulum and Golgi.

The Journal of biological chemistry

Tóth B, Balla A, Ma H, Knight ZA, Shokat KM, Balla T

JNK2 is a positive regulator of the cJun transcription factor.

Molecular cell

Jaeschke A, Karasarides M, Ventura JJ, Ehrhardt A, Zhang C, Flavell RA, Shokat KM, Davis RJ

To stabilize neutrophil polarity, PIP3 and Cdc42 augment RhoA activity at the back as well as signals at the front.

The Journal of cell biology

Van Keymeulen A, Wong K, Knight ZA, Govaerts C, Hahn KM, Shokat KM, Bourne HR

Arabidopsis MAP kinase 4 regulates salicylic acid- and jasmonic acid/ethylene-dependent responses via EDS1 and PAD4.

The Plant journal : for cell and molecular biology

Brodersen P, Petersen M, Bjørn Nielsen H, Zhu S, Newman MA, Shokat KM, Rietz S, Parker J, Mundy J

A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma.

Cancer cell

Fan QW, Knight ZA, Goldenberg DD, Yu W, Mostov KE, Stokoe D, Shokat KM, Weiss WA

A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling.

Cell

Knight ZA, Gonzalez B, Feldman ME, Zunder ER, Goldenberg DD, Williams O, Loewith R, Stokoe D, Balla A, Toth B, Balla T, Weiss WA, Williams RL, Shokat KM

Effect of combined DNA repair inhibition and G2 checkpoint inhibition on cell cycle progression after DNA damage.

Molecular cancer therapeutics

Sturgeon CM, Knight ZA, Shokat KM, Roberge M

Selective kinase inhibition by exploiting differential pathway sensitivity.

Chemistry & biology

Kung C, Kenski DM, Krukenberg K, Madhani HD, Shokat KM

Chemical genetic analysis of the time course of signal transduction by JNK.

Molecular cell

Ventura JJ, Hübner A, Zhang C, Flavell RA, Shokat KM, Davis RJ

The cyclin-dependent kinase (CDK) family member PNQALRE/CCRK supports cell proliferation but has no intrinsic CDK-activating kinase (CAK) activity.

Cell cycle (Georgetown, Tex.)

Wohlbold L, Larochelle S, Liao JC, Livshits G, Singer J, Shokat KM, Fisher RP

Combining chemical genetics and proteomics to identify protein kinase substrates.

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

Dephoure N, Howson RW, Blethrow JD, Shokat KM, O'Shea EK

Dichotomous but stringent substrate selection by the dual-function Cdk7 complex revealed by chemical genetics.

Nature structural & molecular biology

Larochelle S, Batliner J, Gamble MJ, Barboza NM, Kraybill BC, Blethrow JD, Shokat KM, Fisher RP

Chemical genetic engineering of G protein-coupled receptor kinase 2.

The Journal of biological chemistry

Kenski DM, Zhang C, von Zastrow M, Shokat KM

The protein kinase Kin4 inhibits exit from mitosis in response to spindle position defects.

Molecular cell

D'Aquino KE, Monje-Casas F, Paulson J, Reiser V, Charles GM, Lai L, Shokat KM, Amon A

A second-site suppressor strategy for chemical genetic analysis of diverse protein kinases.

Nature methods

Zhang C, Kenski DM, Paulson JL, Bonshtien A, Sessa G, Cross JV, Templeton DJ, Shokat KM

Features of selective kinase inhibitors.

Chemistry & biology

Knight ZA, Shokat KM

Structural bioinformatics-based design of selective, irreversible kinase inhibitors.

Science (New York, N.Y.)

Cohen MS, Zhang C, Shokat KM, Taunton J

Bio-orthogonal affinity purification of direct kinase substrates.

Journal of the American Chemical Society

Allen JJ, Lazerwith SE, Shokat KM

Targeting the gatekeeper residue in phosphoinositide 3-kinases.

Bioorganic & medicinal chemistry

Alaimo PJ, Knight ZA, Shokat KM

A chemical-genetic approach to studying neurotrophin signaling.

Neuron

Chen X, Ye H, Kuruvilla R, Ramanan N, Scangos KW, Zhang C, Johnson NM, England PM, Shokat KM, Ginty DD

An unbiased cell morphology-based screen for new, biologically active small molecules.

PLoS biology

Tanaka M, Bateman R, Rauh D, Vaisberg E, Ramachandani S, Zhang C, Hansen KC, Burlingame AL, Trautman JK, Shokat KM, Adams CL

Small-molecule kinase-inhibitor target assessment.

Chembiochem : a European journal of chemical biology

Kung C, Shokat KM

Chemical genomic profiling to identify intracellular targets of a multiplex kinase inhibitor.

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

Kung C, Kenski DM, Dickerson SH, Howson RW, Kuyper LF, Madhani HD, Shokat KM

Chemical genetics reveals a role for Mps1 kinase in kinetochore attachment during mitosis.

Current biology : CB

Jones MH, Huneycutt BJ, Pearson CG, Zhang C, Morgan G, Shokat K, Bloom K, Winey M

Isoform-specific phosphoinositide 3-kinase inhibitors from an arylmorpholine scaffold.

Bioorganic & medicinal chemistry

Knight ZA, Chiang GG, Alaimo PJ, Kenski DM, Ho CB, Coan K, Abraham RT, Shokat KM

A mechanism-based cross-linker for the identification of kinase-substrate pairs.

Journal of the American Chemical Society

Maly DJ, Allen JA, Shokat KM

Rapid structure-activity and selectivity analysis of kinase inhibitors by BioMAP analysis in complex human primary cell-based models.

Assay and drug development technologies

Kunkel EJ, Plavec I, Nguyen D, Melrose J, Rosler ES, Kao LT, Wang Y, Hytopoulos E, Bishop AC, Bateman R, Shokat KM, Butcher EC, Berg EL

A phage display selection of engrailed homeodomain mutants and the importance of residue Q50.

Nucleic acids research

Simon MD, Sato K, Weiss GA, Shokat KM

Dissecting the Engrailed homeodomain-DNA interaction by phage-displayed shotgun scanning.

Chemistry & biology

Sato K, Simon MD, Levin AM, Shokat KM, Weiss GA

Design and use of analog-sensitive protein kinases.

Current protocols in molecular biology

Blethrow J, Zhang C, Shokat KM, Weiss EL

Chemical-genetic inhibition of a sensitized mutant myosin Vb demonstrates a role in peripheral-pericentriolar membrane traffic.

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

Provance DW, Gourley CR, Silan CM, Cameron LC, Shokat KM, Goldenring JR, Shah K, Gillespie PG, Mercer JA

Two cyclin-dependent kinases promote RNA polymerase II transcription and formation of the scaffold complex.

Molecular and cellular biology

Liu Y, Kung C, Fishburn J, Ansari AZ, Shokat KM, Hahn S

Engineering the serine/threonine protein kinase Raf-1 to utilise an orthogonal analogue of ATP substituted at the N6 position.

FEBS letters

Hindley AD, Park S, Wang L, Shah K, Wang Y, Hu X, Shokat KM, Kolch W, Sedivy JM, Yeung KC

Combinatorial efficacy achieved through two-point blockade within a signaling pathway-a chemical genetic approach.

Cancer research

Fan QW, Specht KM, Zhang C, Goldenberg DD, Shokat KM, Weiss WA

Mek1 kinase activity functions downstream of RED1 in the regulation of meiotic double strand break repair in budding yeast.

Molecular biology of the cell

Wan L, de los Santos T, Zhang C, Shokat K, Hollingsworth NM

Targets of the cyclin-dependent kinase Cdk1.

Nature

Ubersax JA, Woodbury EL, Quang PN, Paraz M, Blethrow JD, Shah K, Shokat KM, Morgan DO

Bypassing a kinase activity with an ATP-competitive drug.

Science (New York, N.Y.)

Papa FR, Zhang C, Shokat K, Walter P

Dynamic phosphoregulation of the cortical actin cytoskeleton and endocytic machinery revealed by real-time chemical genetic analysis.

The Journal of cell biology

Sekiya-Kawasaki M, Groen AC, Cope MJ, Kaksonen M, Watson HA, Zhang C, Shokat KM, Wendland B, McDonald KL, McCaffery JM, Drubin DG

Specific inhibition of Elm1 kinase activity reveals functions required for early G1 events.

Molecular and cellular biology

Sreenivasan A, Bishop AC, Shokat KM, Kellogg DR

Phosphospecific proteolysis for mapping sites of protein phosphorylation.

Nature biotechnology

Knight ZA, Schilling B, Row RH, Kenski DM, Gibson BW, Shokat KM

Cutting edge: a chemical genetic system for the analysis of kinases regulating T cell development.

Journal of immunology (Baltimore, Md. : 1950)

Denzel A, Hare KJ, Zhang C, Shokat K, Jenkinson EJ, Anderson G, Hayday A

Control of landmark events in meiosis by the CDK Cdc28 and the meiosis-specific kinase Ime2.

Genes & development

Benjamin KR, Zhang C, Shokat KM, Herskowitz I

Inducible protein knockout reveals temporal requirement of CaMKII reactivation for memory consolidation in the brain.

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

Wang H, Shimizu E, Tang YP, Cho M, Kyin M, Zuo W, Robinson DA, Alaimo PJ, Zhang C, Morimoto H, Zhuo M, Feng R, Shokat KM, Tsien JZ

Identification of novel ERK2 substrates through use of an engineered kinase and ATP analogs.

The Journal of biological chemistry

Eblen ST, Kumar NV, Shah K, Henderson MJ, Watts CK, Shokat KM, Weber MJ

Chemical genetic analysis of Apg1 reveals a non-kinase role in the induction of autophagy.

Molecular biology of the cell

Abeliovich H, Zhang C, Dunn WA, Shokat KM, Klionsky DJ

A chemical genetic approach for the identification of direct substrates of protein kinases.

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

Shah K, Shokat KM

Conformational restraint is a critical determinant of unnatural nucleotide recognition by protein kinases.

Bioorganic & medicinal chemistry letters

Ulrich SM, Sallee NA, Shokat KM

Inhibitor scaffolds as new allele specific kinase substrates.

Journal of the American Chemical Society

Kraybill BC, Elkin LL, Blethrow JD, Morgan DO, Shokat KM

A kinase sequence database: sequence alignments and family assignment.

Bioinformatics (Oxford, England)

Buzko O, Shokat KM

Protein engineering of protein kinase A catalytic subunits results in the acquisition of novel inhibitor sensitivity.

The Journal of biological chemistry

Niswender CM, Ishihara RW, Judge LM, Zhang C, Shokat KM, McKnight GS

The emerging power of chemical genetics.

Current opinion in cell biology

Specht KM, Shokat KM

A chemical-genetic strategy implicates myosin-1c in adaptation by hair cells.

Cell

Holt JR, Gillespie SK, Provance DW, Shah K, Shokat KM, Corey DP, Mercer JA, Gillespie PG

Chemical Genetic Analysis of Protein Kinase Cascades.

TheScientificWorldJournal

Alaimo PJ, Shogren-Knaak MA, Shokat KM

Modified AutoDock for accurate docking of protein kinase inhibitors.

Journal of computer-aided molecular design

Buzko OV, Bishop AC, Shokat KM

Green fluorescent protein-based protein kinase biosensor substrates.

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

Ulrich S, Shokat K