
Professor
M_CMP (Cellular Molecular Pha)
+1 415 514-0472
Publications
The structure of KRASG12C bound to divarasib highlights features of potent switch-II pocket engagement.
Small GTPases
Deazaguanylation is a nucleobase-protein conjugation required for type IV CBASS immunity.
bioRxiv : the preprint server for biology
Direct RAS inhibitors turn 10.
Nature chemical biology
Subcellular activation of β-adrenergic receptors using a spatially restricted antagonist.
Proceedings of the National Academy of Sciences of the United States of America
IL-13 and IL-17A activate ß1 integrin through an NF-kB/Rho kinase/PIP5K1? pathway to enhance force transmission in airway smooth muscle.
Proceedings of the National Academy of Sciences of the United States of America
Acute rapamycin treatment reveals novel mechanisms of behavioral, physiological, and functional dysfunction in a maternal inflammation mouse model of autism and sensory over-responsivity.
bioRxiv : the preprint server for biology
IL-13 and IL-17A Activate β1 Integrin through an NF-kB/Rho kinase/PIP5K1γ pathway to Enhance Force Transmission in Airway Smooth Muscle.
bioRxiv : the preprint server for biology
Strain-release alkylation of Asp12 enables mutant selective targeting of K-Ras-G12D.
Nature chemical biology
Nanomolar Protein Thermal Profiling with Modified Cyanine Dyes.
Analytical chemistry
Selective activation of intracellular β1AR using a spatially restricted antagonist.
bioRxiv : the preprint server for biology
Protocol for performing and optimizing differential scanning fluorimetry experiments.
STAR protocols
Proteomic and genetic analyses of influenza A viruses identify pan-viral host targets.
Nature communications
Direct Modulators of K-Ras-Membrane Interactions.
ACS chemical biology
Chemical Genetic Identification of Protein Kinase C Epsilon Substrates in Mouse Brain.
Molecular & cellular proteomics : MCP
A Small Molecule Reacts with the p53 Somatic Mutant Y220C to Rescue Wild-type Thermal Stability.
Cancer discovery
IFITM proteins assist cellular uptake of diverse linked chemotypes.
Science (New York, N.Y.)
Probing the KRas Switch II Groove by Fluorine NMR Spectroscopy.
ACS chemical biology
Cold shock domain-containing protein E1 is a posttranscriptional regulator of the LDL receptor.
Science translational medicine
Tissue-restricted inhibition of mTOR using chemical genetics.
Proceedings of the National Academy of Sciences of the United States of America
Chemoselective Covalent Modification of K-Ras(G12R) with a Small Molecule Electrophile.
Journal of the American Chemical Society
Chemical acylation of an acquired serine suppresses oncogenic signaling of K-Ras(G12S).
Nature chemical biology
CD74-NRG1 fusions are oncogenic in vivo and induce therapeutically tractable ERBB2:ERBB3 heterodimerization.
Molecular cancer therapeutics
KRAS is vulnerable to reversible switch-II pocket engagement in cells.
Nature chemical biology
Drugging the Next Undruggable KRAS Allele-Gly12Asp.
Journal of medicinal chemistry
Drugging the undruggable: Ross Cagan interviews Kevan Shokat.
Disease models & mechanisms
Dissecting the biology of mTORC1 beyond rapamycin.
Science signaling
Brain-specific inhibition of mTORC1 eliminates side effects resulting from mTORC1 blockade in the periphery and reduces alcohol intake in mice.
Nature communications
Drug-induced phospholipidosis confounds drug repurposing for SARS-CoV-2.
Science (New York, N.Y.)
Evolution of enhanced innate immune evasion by the SARS-CoV-2 B.1.1.7 UK variant.
bioRxiv : the preprint server for biology
Phospholipidosis is a shared mechanism underlying the in vitro antiviral activity of many repurposed drugs against SARS-CoV-2.
bioRxiv : the preprint server for biology
Spermatogonial Stem Cell Numbers Are Reduced by Transient Inhibition of GDNF Signaling but Restored by Self-Renewing Replication when Signaling Resumes.
Stem cell reports
Host-directed therapies against early-lineage SARS-CoV-2 retain efficacy against B.1.1.7 variant.
bioRxiv : the preprint server for biology
Drugging the 'undruggable' MYCN oncogenic transcription factor: Overcoming previous obstacles to impact childhood cancers.
Cancer research
Plitidepsin has potent preclinical efficacy against SARS-CoV-2 by targeting the host protein eEF1A.
Science (New York, N.Y.)
Comparative host-coronavirus protein interaction networks reveal pan-viral disease mechanisms.
Science (New York, N.Y.)
GTP-State-Selective Cyclic Peptide Ligands of K-Ras(G12D) Block Its Interaction with Raf.
ACS central science
The splicing modulator sulfonamide indisulam reduces AR-V7 in prostate cancer cells.
Bioorganic & medicinal chemistry
Unbiased Proteomic Profiling Uncovers a Targetable GNAS/PKA/PP2A Axis in Small Cell Lung Cancer Stem Cells.
Cancer cell
Betacellulin drives therapy-resistance in glioblastoma.
Neuro-Oncology
A SARS-CoV-2-Human Protein-Protein Interaction Map Reveals Drug Targets and Potential Drug-Repurposing.
bioRxiv : the preprint server for biology
PI4KIIIß is a therapeutic target in chromosome 1q-amplified lung adenocarcinoma.
Science translational medicine
p27 allosterically activates cyclin-dependent kinase 4 and antagonizes palbociclib inhibition.
Science (New York, N.Y.)
p38? MAPK contributes to left ventricular remodeling after pathologic stress and disinhibits calpain through phosphorylation of calpastatin.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology
Bifunctional Small-Molecule Ligands of K-Ras Induce Its Association with Immunophilin Proteins.
Angewandte Chemie (International ed. in English)
KRASG12C inhibition produces a driver-limited state revealing collateral dependencies.
Science signaling
Phosphoregulation of the oncogenic protein regulator of cytokinesis 1 (PRC1) by the atypical CDK16/CCNY complex.
Experimental & molecular medicine
A Legionella pneumophila Kinase Phosphorylates the Hsp70 Chaperone Family to Inhibit Eukaryotic Protein Synthesis.
Cell host & microbe
Chronic TGF-ß exposure drives stabilized EMT, tumor stemness, and cancer drug resistance with vulnerability to bitopic mTOR inhibition.
Science signaling
Chemically reprogramming the phospho-transfer reaction to crosslink protein kinases to their substrates.
Protein science : a publication of the Protein Society
Type II kinase inhibitors targeting Cys-gatekeeper kinases display orthogonality with wild type and Ala/Gly-gatekeeper kinases.
ACS chemical biology
Chemical genetic inhibition of DEAD-box proteins using covalent complementarity.
Nucleic acids research
A Patient-derived Xenograft Model of Pancreatic Neuroendocrine Tumors Identifies Sapanisertib as a Possible New Treatment for Everolimus-Resistant Tumors.
Molecular cancer therapeutics
A High-Throughput Luciferase Assay to Evaluate Proteolysis of the Single-Turnover Protease PCSK9.
Journal of visualized experiments : JoVE
Kinome rewiring reveals AURKA limits PI3K-pathway inhibitor efficacy in breast cancer.
Nature chemical biology
Stepwise processing analyses of the single-turnover PCSK9 protease reveal its substrate sequence specificity and link clinical genotype to lipid phenotype.
The Journal of biological chemistry
Novel K-Ras G12C Switch-II Covalent Binders Destabilize Ras and Accelerate Nucleotide Exchange.
Journal of chemical information and modeling
Stepwise processing analyses of the single-turnover PCSK9 protease reveal its substrate sequence specificity and link clinical genotype to lipid phenotype.
The Journal of biological chemistry
Ras Binder Induces a Modified Switch-II Pocket in GTP and GDP States.
Cell chemical biology
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
A new generation of mTORC1 inhibitor attenuates alcohol intake and reward in mice.
Addiction biology
Drugging the 'undruggable' cancer targets.
Nature reviews. Cancer
Farnesyltransferase-Mediated Delivery of a Covalent Inhibitor Overcomes Alternative Prenylation to Mislocalize K-Ras.
ACS chemical biology
Drugging the catalytically inactive state of RET kinase in RET-rearranged tumors.
Science translational medicine
Site-specific incorporation of phosphotyrosine using an expanded genetic code.
Nature chemical biology
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
Long-term oral kinetin does not protect against a-synuclein-induced neurodegeneration in rodent models of Parkinson's disease.
Neurochemistry international
INPP4B and PTEN Loss Leads to PI-3,4-P2 Accumulation and Inhibition of PI3K in TNBC.
Molecular cancer research : MCR
An Optimized Chromatographic Strategy for Multiplexing In Parallel Reaction Monitoring Mass Spectrometry: Insights from Quantitation of Activated Kinases.
Molecular & cellular proteomics : MCP
Endosomal Phosphatidylinositol 3-Kinase Is Essential for Canonical GPCR Signaling.
Molecular pharmacology
Discovery of new substrates of the elongation factor-2 kinase suggests a broader role in the cellular nutrient response.
Cellular signalling
Overcoming resistance to HER2 inhibitors through state-specific kinase binding.
Nature chemical biology
From Powerful Review Articles to Research Breakthroughs.
Cell chemical biology
Inhibition of Carbonyl Reductase 1 Safely Improves the Efficacy of Doxorubicin in Breast Cancer Treatment.
Antioxidants & redox signaling
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
Direct small-molecule inhibitors of KRAS: from structural insights to mechanism-based design.
Nature reviews. Drug discovery
Synthetic Lethal Targeting of ARID1A-Mutant Ovarian Clear Cell Tumors with Dasatinib.
Molecular cancer therapeutics
Isocitrate Dehydrogenase Mutations Confer Dasatinib Hypersensitivity and SRC Dependence in Intrahepatic Cholangiocarcinoma.
Cancer discovery
Multistep Compositional Remodeling of Supported Lipid Membranes by Interfacially Active Phosphatidylinositol Kinases.
Analytical chemistry
N-Myc Drives Neuroendocrine Prostate Cancer Initiated from Human Prostate Epithelial Cells.
Cancer cell
Our Advisors, Our Ambassadors, Our Editorial Board Members.
Cell chemical biology
Design and Structural Characterization of Potent and Selective Inhibitors of Phosphatidylinositol 4 Kinase IIIß.
Journal of medicinal chemistry
Voices of Chemical Biology: Charting the Next Decade.
Cell chemical biology
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
Cell Chemical Biology: Home of Exciting Chemical Biology.
Cell chemical biology
P-TEFb regulation of transcription termination factor Xrn2 revealed by a chemical genetic screen for Cdk9 substrates.
Genes & development
Analog sensitive chemical inhibition of the DEAD-box protein DDX3.
Protein science : a publication of the Protein Society
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
Discovery and functional characterization of a neomorphic PTEN mutation.
Proceedings of the National Academy of Sciences of the United States of America
Discovery and structure of a new inhibitor scaffold of the autophagy initiating kinase ULK1.
Bioorganic & medicinal chemistry
SR protein kinases promote splicing of nonconsensus introns.
Nature structural & molecular biology
WNK1-regulated inhibitory phosphorylation of the KCC2 cotransporter maintains the depolarizing action of GABA in immature neurons.
Science signaling
Downregulation of MYCN through PI3K Inhibition in Mouse Models of Pediatric Neural Cancer.
Frontiers in oncology
Differential genetic interactions of yeast stress response MAPK pathways.
Molecular systems biology
The Tribbles 2 (TRB2) pseudokinase binds to ATP and autophosphorylates in a metal-independent manner.
The Biochemical journal
Structure of the human autophagy initiating kinase ULK1 in complex with potent inhibitors.
ACS chemical biology
Radiotherapy followed by aurora kinase inhibition targets tumor-propagating cells in human glioblastoma.
Molecular cancer therapeutics
Targeting osteosarcoma.
Proceedings of the National Academy of Sciences of the United States of America
Linking tumor mutations to drug responses via a quantitative chemical-genetic interaction map.
Cancer discovery
Reflecting on the past and looking forward to the future of bridging chemistry and biology.
Chemistry & biology
The proprotein convertase subtilisin/kexin type 9 (PCSK9) active site and cleavage sequence differentially regulate protein secretion from proteolysis.
The Journal of biological chemistry
TrkB kinase activity maintains synaptic function and structural integrity at adult neuromuscular junctions.
Journal of applied physiology (Bethesda, Md. : 1985)
Responses to glial cell line-derived neurotrophic factor change in mice as spermatogonial stem cells form progenitor spermatogonia which replicate and give rise to more differentiated progeny.
Biology of reproduction
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
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
Quantitative and temporal requirements revealed for Zap70 catalytic activity during T cell development.
Nature immunology
Structures of PI4KIIIß complexes show simultaneous recruitment of Rab11 and its effectors.
Science (New York, N.Y.)
A crosslinker based on a tethered electrophile for mapping kinase-substrate networks.
Chemistry & biology
Methods in Enzymology. Protein kinase inhibitors in research and medicine. Preface.
Methods in enzymology
The logic and design of analog-sensitive kinases and their small molecule inhibitors.
Methods in enzymology
Inhibition of the kinase Csk in thymocytes reveals a requirement for actin remodeling in the initiation of full TCR signaling.
Nature immunology
PLC-? and PI3K link cytokines to ERK activation in hematopoietic cells with normal and oncogenic Kras.
Science signaling
Generation of a patient-derived chordoma xenograft and characterization of the phosphoproteome in a recurrent chordoma.
Journal of neurosurgery
Staurosporine-derived inhibitors broaden the scope of analog-sensitive kinase technology.
Journal of the American Chemical Society
EGFR phosphorylates tumor-derived EGFRvIII driving STAT3/5 and progression in glioblastoma.
Cancer cell
Structure-guided inhibitor design expands the scope of analog-sensitive kinase technology.
ACS chemical biology
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
PTEN expression is consistent in colorectal cancer primaries and metastases and associates with patient survival.
Cancer medicine
Optimizing small molecule inhibitors of calcium-dependent protein kinase 1 to prevent infection by Toxoplasma gondii.
Journal of medicinal chemistry
Glucose sensor O-GlcNAcylation coordinates with phosphorylation to regulate circadian clock.
Cell metabolism
News from the Chemistry & Biology editorial team.
Chemistry & biology
A chemical genetic approach reveals distinct EphB signaling mechanisms during brain development.
Nature neuroscience
Cyclin-dependent kinase control of the initiation-to-elongation switch of RNA polymerase II.
Nature structural & molecular biology
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
Integrin a9ß1 in airway smooth muscle suppresses exaggerated airway narrowing.
The Journal of clinical investigation
The AMP-activated protein kinase Snf1 regulates transcription factor binding, RNA polymerase II activity, and mRNA stability of glucose-repressed genes in Saccharomyces cerevisiae.
The Journal of biological chemistry
Carbonyl reductase 1 offers a novel therapeutic target to enhance leukemia treatment by arsenic trioxide.
Cancer research
Orm protein phosphoregulation mediates transient sphingolipid biosynthesis response to heat stress via the Pkh-Ypk and Cdc55-PP2A pathways.
Molecular biology of the cell
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
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
The in vivo response of stem and other undifferentiated spermatogonia to the reversible inhibition of glial cell line-derived neurotrophic factor signaling in the adult.
Stem cells (Dayton, Ohio)
Kinetics of inhibitor cycling underlie therapeutic disparities between EGFR-driven lung and brain cancers.
Cancer discovery
Combination of ATP-competitive mammalian target of rapamycin inhibitors with standard chemotherapy for colorectal cancer.
Investigational new drugs
Development of a chemical genetic approach for human aurora B kinase identifies novel substrates of the chromosomal passenger complex.
Molecular & cellular proteomics : MCP
A method to site-specifically incorporate methyl-lysine analogues into recombinant proteins.
Methods in enzymology
Covalent cross-linking of kinases with their corresponding peptide substrates.
Methods in molecular biology (Clifton, N.J.)
Chemical genetic screen for AMPKa2 substrates uncovers a network of proteins involved in mitosis.
Molecular cell
Generation of a set of conditional analog-sensitive alleles of essential protein kinases in the fission yeast Schizosaccharomyces pombe.
Cell cycle (Georgetown, Tex.)
Genetic deletion of trkB.T1 increases neuromuscular function.
American journal of physiology. Cell physiology
The Cryptosporidium parvum kinome.
BMC genomics
Feedback circuits monitor and adjust basal Lck-dependent events in T cell receptor signaling.
Science signaling
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
Chemical genetic strategy for targeting protein kinases based on covalent complementarity.
Proceedings of the National Academy of Sciences of the United States of America
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
Autophagy suppression promotes apoptotic cell death in response to inhibition of the PI3K-mTOR pathway in pancreatic adenocarcinoma.
Journal of molecular medicine (Berlin, Germany)
Switching Cdk2 on or off with small molecules to reveal requirements in human cell proliferation.
Molecular cell
Chemistry & Biology editors announce changes to the editorial team.
Chemistry & biology
Dose-dependent effects of focal fractionated irradiation on secondary malignant neoplasms in Nf1 mutant mice.
Cancer research
Sensitizing plant protein kinases to specific inhibition by ATP-competitive molecules.
Methods in molecular biology (Clifton, N.J.)
The evolution of protein kinase inhibitors from antagonists to agonists of cellular signaling.
Annual review of biochemistry
Phosphoproteomic analysis reveals interconnected system-wide responses to perturbations of kinases and phosphatases in yeast.
Science signaling
Rewiring of genetic networks in response to DNA damage.
Science (New York, N.Y.)
Constitutive mTORC1 activation by a herpesvirus Akt surrogate stimulates mRNA translation and viral replication.
Genes & development
A genetically selective inhibitor demonstrates a function for the kinase Zap70 in regulatory T cells independent of its catalytic activity.
Nature immunology
A kinase cascade leading to Rab11-FIP5 controls transcytosis of the polymeric immunoglobulin receptor.
Nature cell biology
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
Biocompatibility and reduced drug absorption of sol-gel-treated poly(dimethyl siloxane) for microfluidic cell culture applications.
Analytical chemistry
Human carbonyl reductase 1 upregulated by hypoxia renders resistance to apoptosis in hepatocellular carcinoma cells.
Journal of hepatology
Chemical-genomic dissection of the CTD code.
Nature structural & molecular biology
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
Synthesis and evaluation of indazole based analog sensitive Akt inhibitors.
Molecular bioSystems
Shaping development of autophagy inhibitors with the structure of the lipid kinase Vps34.
Science (New York, N.Y.)
mTOR complex-2 activates ENaC by phosphorylating SGK1.
Journal of the American Society of Nephrology : JASN
Chemical genetic approach for kinase-substrate mapping by covalent capture of thiophosphopeptides and analysis by mass spectrometry.
Current protocols in chemical biology
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
The p110delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors.
Nature chemical biology
Discovery of dual inhibitors of the immune cell PI3Ks p110delta and p110gamma: a prototype for new anti-inflammatory drugs.
Chemistry & biology
Dynamic regulation of a metabolic multi-enzyme complex by protein kinase CK2.
The Journal of biological chemistry
Targeting the cancer kinome through polypharmacology.
Nature reviews. Cancer
The p110 delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors.
Nature chemical biology
Resiliency and vulnerability in the HER2-HER3 tumorigenic driver.
Science translational medicine
New inhibitors of the PI3K-Akt-mTOR pathway: insights into mTOR signaling from a new generation of Tor Kinase Domain Inhibitors (TORKinibs).
Current topics in microbiology and immunology
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
Arterial-venous segregation by selective cell sprouting: an alternative mode of blood vessel formation.
Science (New York, N.Y.)
Use of a semisynthetic epitope to probe histidine kinase activity and regulation.
Analytical biochemistry
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
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
Phosphorylation of the transcription elongation factor Spt5 by yeast Bur1 kinase stimulates recruitment of the PAF complex.
Molecular and cellular biology
PIKfyve regulation of endosome-linked pathways.
Traffic (Copenhagen, Denmark)
Evolution of phosphoregulation: comparison of phosphorylation patterns across yeast species.
PLoS biology
Inhibitor hijacking of Akt activation.
Nature chemical biology
Tuning the activation threshold of a kinase network by nested feedback loops.
Science (New York, N.Y.)
Bypassing kinase activity of the tomato Pto resistance protein with small molecule ligands.
The Journal of biological chemistry
TFIIH and P-TEFb coordinate transcription with capping enzyme recruitment at specific genes in fission yeast.
Molecular cell
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
Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2.
PLoS biology
A complex-based reconstruction of the Saccharomyces cerevisiae interactome.
Molecular & cellular proteomics : MCP
EGFR signals to mTOR through PKC and independently of Akt in glioma.
Science signaling
Generation of a novel system for studying spleen tyrosine kinase function in macrophages and B cells.
Journal of immunology (Baltimore, Md. : 1950)
Tuning a three-component reaction for trapping kinase substrate complexes.
Journal of the American Chemical Society
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
Distinct activation pathways confer cyclin-binding specificity on Cdk1 and Cdk2 in human cells.
Molecular cell
Distinct roles of class IA PI3K isoforms in primary and immortalised macrophages.
Journal of cell science
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
A chemical genomics study identifies Snf1 as a repressor of GCN4 translation.
The Journal of biological chemistry
Small molecule recognition of c-Src via the Imatinib-binding conformation.
Chemistry & biology
Dual inhibition of PI3Kalpha and mTOR as an alternative treatment for Kaposi's sarcoma.
Cancer research
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.
Nature chemical biology
The yeast LATS/Ndr kinase Cbk1 regulates growth via Golgi-dependent glycosylation and secretion.
Molecular biology of the cell
A chemical screen in diverse breast cancer cell lines reveals genetic enhancers and suppressors of sensitivity to PI3K isoform-selective inhibition.
The Biochemical journal
Genetic or pharmaceutical blockade of p110delta phosphoinositide 3-kinase enhances IgE production.
The Journal of allergy and clinical immunology
PIK3CA cooperates with other phosphatidylinositol 3'-kinase pathway mutations to effect oncogenic transformation.
Cancer research
Human carbonyl reductase 1 is an S-nitrosoglutathione reductase.
The Journal of biological chemistry
A chemical-genetic strategy reveals distinct temporal requirements for SAD-1 kinase in neuronal polarization and synapse formation.
Neural development
The effect of H3K79 dimethylation and H4K20 trimethylation on nucleosome and chromatin structure.
Nature structural & molecular biology
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
Discovery of drug-resistant and drug-sensitizing mutations in the oncogenic PI3K isoform p110 alpha.
Cancer cell
The brain-derived neurotrophic factor receptor TrkB is critical for the acquisition but not expression of conditioned incentive value.
The European journal of neuroscience
Activity of the p110-alpha subunit of phosphatidylinositol-3-kinase is required for activation of epithelial sodium transport.
American journal of physiology. Renal physiology
An integrated platform of genomic assays reveals small-molecule bioactivities.
Nature chemical biology
Nuclear HuR accumulation through phosphorylation by Cdk1.
Genes & development
Hyperphosphorylation of RNA polymerase II in response to topoisomerase I cleavage complexes and its association with transcription- and BRCA1-dependent degradation of topoisomerase I.
Journal of molecular biology
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
Analysis of 3-phosphoinositide-dependent kinase-1 signaling and function in ES cells.
Experimental cell research
Characterization of structurally distinct, isoform-selective phosphoinositide 3'-kinase inhibitors in combination with radiation in the treatment of glioblastoma.
Molecular cancer therapeutics
Inhibition of ZAP-70 kinase activity via an analog-sensitive allele blocks T cell receptor and CD28 superagonist signaling.
The Journal of biological chemistry
Cdc28-Clb5 (CDK-S) and Cdc7-Dbf4 (DDK) collaborate to initiate meiotic recombination in yeast.
Genes & development
Covalent capture of kinase-specific phosphopeptides reveals Cdk1-cyclin B substrates.
Proceedings of the National Academy of Sciences of the United States of America
Design of drug-resistant alleles of type-III phosphatidylinositol 4-kinases using mutagenesis and molecular modeling.
Biochemistry
Maintenance of hormone-sensitive phosphoinositide pools in the plasma membrane requires phosphatidylinositol 4-kinase IIIalpha.
Molecular biology of the cell
Recognizing and exploiting differences between RNAi and small-molecule inhibitors.
Nature chemical biology
IRE1 signaling affects cell fate during the unfolded protein response.
Science (New York, N.Y.)
Access denied: Snf1 activation loop phosphorylation is controlled by availability of the phosphorylated threonine 210 to the PP1 phosphatase.
The Journal of biological chemistry
A coupled chemical-genetic and bioinformatic approach to Polo-like kinase pathway exploration.
Chemistry & biology
A surface on the androgen receptor that allosterically regulates coactivator binding.
Proceedings of the National Academy of Sciences of the United States of America
Suppression of p53-dependent senescence by the JNK signal transduction pathway.
Proceedings of the National Academy of Sciences of the United States of America
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
A remodelled protease that cleaves phosphotyrosine substrates.
Journal of the American Chemical Society
A dual phosphoinositide-3-kinase alpha/mTOR inhibitor cooperates with blockade of epidermal growth factor receptor in PTEN-mutant glioma.
Cancer research
Glutathione traps formaldehyde by formation of a bicyclo[4.4.1]undecane adduct.
Organic & biomolecular chemistry
A semisynthetic epitope for kinase substrates.
Nature methods
HIV-1 Nef assembles a Src family kinase-ZAP-70/Syk-PI3K cascade to downregulate cell-surface MHC-I.
Cell host & microbe
Chemically targeting the PI3K family.
Biochemical Society transactions
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
Requirements for Cdk7 in the assembly of Cdk1/cyclin B and activation of Cdk2 revealed by chemical genetics in human cells.
Molecular cell
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
Structure-guided development of affinity probes for tyrosine kinases using chemical genetics.
Nature chemical biology
A membrane capture assay for lipid kinase activity.
Nature protocols
Construction of conditional analog-sensitive kinase alleles in the fission yeast Schizosaccharomyces pombe.
Nature protocols
Structure and properties of a re-engineered homeodomain protein-DNA interface.
ACS chemical biology
Phosphatidylinositol 4-kinase IIIbeta regulates the transport of ceramide between the endoplasmic reticulum and Golgi.
The Journal of biological chemistry
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
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
Forebrain overexpression of CaMKII abolishes cingulate long term depression and reduces mechanical allodynia and thermal hyperalgesia.
Molecular pain
Chemical genomics: dialed in transcriptional network control with non-steroidal glucocorticoid receptor modulators.
ACS chemical biology
Effect of combined DNA repair inhibition and G2 checkpoint inhibition on cell cycle progression after DNA damage.
Molecular cancer therapeutics
Selective kinase inhibition by exploiting differential pathway sensitivity.
Chemistry & biology
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.)
Combining chemical genetics and proteomics to identify protein kinase substrates.
Proceedings of the National Academy of Sciences of the United States of America
Dichotomous but stringent substrate selection by the dual-function Cdk7 complex revealed by chemical genetics.
Nature structural & molecular biology
The Ipl1-Aurora protein kinase activates the spindle checkpoint by creating unattached kinetochores.
Nature cell biology
Chemical genetic engineering of G protein-coupled receptor kinase 2.
The Journal of biological chemistry
The protein kinase Kin4 inhibits exit from mitosis in response to spindle position defects.
Molecular cell
A second-site suppressor strategy for chemical genetic analysis of diverse protein kinases.
Nature methods
Features of selective kinase inhibitors.
Chemistry & biology
Structural bioinformatics-based design of selective, irreversible kinase inhibitors.
Science (New York, N.Y.)
Bio-orthogonal affinity purification of direct kinase substrates.
Journal of the American Chemical Society
Targeting the gatekeeper residue in phosphoinositide 3-kinases.
Bioorganic & medicinal chemistry
Small-molecule kinase-inhibitor target assessment.
Chembiochem : a European journal of chemical biology
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
Chemical genetics reveals a role for Mps1 kinase in kinetochore attachment during mitosis.
Current biology : CB
Sole BCR-ABL inhibition is insufficient to eliminate all myeloproliferative disorder cell populations.
Proceedings of the National Academy of Sciences of the United States of America
Isoform-specific phosphoinositide 3-kinase inhibitors from an arylmorpholine scaffold.
Bioorganic & medicinal chemistry
A mechanism-based cross-linker for the identification of kinase-substrate pairs.
Journal of the American Chemical Society
Rapid structure-activity and selectivity analysis of kinase inhibitors by BioMAP analysis in complex human primary cell-based models.
Assay and drug development technologies
A phage display selection of engrailed homeodomain mutants and the importance of residue Q50.
Nucleic acids research
Adaptability at a protein-DNA interface: re-engineering the engrailed homeodomain to recognize an unnatural nucleotide.
Journal of the American Chemical Society
Dissecting the Engrailed homeodomain-DNA interaction by phage-displayed shotgun scanning.
Chemistry & biology
Design and use of analog-sensitive protein kinases.
Current protocols in molecular biology
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
Two cyclin-dependent kinases promote RNA polymerase II transcription and formation of the scaffold complex.
Molecular and cellular biology
Combinatorial efficacy achieved through two-point blockade within a signaling pathway-a chemical genetic approach.
Cancer research
Mek1 kinase activity functions downstream of RED1 in the regulation of meiotic double strand break repair in budding yeast.
Molecular biology of the cell
Bypassing a kinase activity with an ATP-competitive drug.
Science (New York, N.Y.)
Dynamic phosphoregulation of the cortical actin cytoskeleton and endocytic machinery revealed by real-time chemical genetic analysis.
The Journal of cell biology
Specific inhibition of Elm1 kinase activity reveals functions required for early G1 events.
Molecular and cellular biology
Phosphospecific proteolysis for mapping sites of protein phosphorylation.
Nature biotechnology
Cutting edge: a chemical genetic system for the analysis of kinases regulating T cell development.
Journal of immunology (Baltimore, Md. : 1950)
Engineering a "methionine clamp" into Src family kinases enhances specificity toward unnatural ATP analogues.
Biochemistry
Control of landmark events in meiosis by the CDK Cdc28 and the meiosis-specific kinase Ime2.
Genes & development
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
Identification of novel ERK2 substrates through use of an engineered kinase and ATP analogs.
The Journal of biological chemistry
Chemical genetic analysis of Apg1 reveals a non-kinase role in the induction of autophagy.
Molecular biology of the cell
A chemical genetic approach for the identification of direct substrates of protein kinases.
Methods in molecular biology (Clifton, N.J.)
Conformational restraint is a critical determinant of unnatural nucleotide recognition by protein kinases.
Bioorganic & medicinal chemistry letters
Inhibitor scaffolds as new allele specific kinase substrates.
Journal of the American Chemical Society
A kinase sequence database: sequence alignments and family assignment.
Bioinformatics (Oxford, England)
The Saccharomyces cerevisiae Mob2p-Cbk1p kinase complex promotes polarized growth and acts with the mitotic exit network to facilitate daughter cell-specific localization of Ace2p transcription factor.
The Journal of cell biology
Chemical genetic blockade of transformation reveals dependence on aberrant oncogenic signaling.
Current biology : CB
Novel chemical genetic approaches to the discovery of signal transduction inhibitors.
Drug discovery today
Protein engineering of protein kinase A catalytic subunits results in the acquisition of novel inhibitor sensitivity.
The Journal of biological chemistry
The emerging power of chemical genetics.
Current opinion in cell biology
Chemical Genetic Analysis of Protein Kinase Cascades.
TheScientificWorldJournal
Modified AutoDock for accurate docking of protein kinase inhibitors.
Journal of computer-aided molecular design
A chemical genetic screen for direct v-Src substrates reveals ordered assembly of a retrograde signaling pathway.
Chemistry & biology
Green fluorescent protein-based protein kinase biosensor substrates.
Methods in molecular biology (Clifton, N.J.)
Mutant tyrosine kinases with unnatural nucleotide specificity retain the structure and phospho-acceptor specificity of the wild-type enzyme.
Chemistry & biology
Chemical inhibition of the Pho85 cyclin-dependent kinase reveals a role in the environmental stress response.
Proceedings of the National Academy of Sciences of the United States of America
Chemical genetic approaches for the elucidation of signaling pathways.
Current opinion in chemical biology
The LuxS family of bacterial autoinducers: biosynthesis of a novel quorum-sensing signal molecule.
Molecular microbiology
Magic bullets for protein kinases.
Trends in cell biology
Identification of new JNK substrate using ATP pocket mutant JNK and a corresponding ATP analogue.
The Journal of biological chemistry
ERK phosphorylation drives cytoplasmic accumulation of hnRNP-K and inhibition of mRNA translation.
Nature cell biology
Recent advances in chemical approaches to the study of biological systems.
Annual review of cell and developmental biology
Chemical genetic analysis of the budding-yeast p21-activated kinase Cla4p.
Nature cell biology
Entry of B cell receptor into signaling domains is inhibited in tolerant B cells.
The Journal of experimental medicine
Unnatural ligands for engineered proteins: new tools for chemical genetics.
Annual review of biophysics and biomolecular structure
Engineering of the myosin-ibeta nucleotide-binding pocket to create selective sensitivity to N(6)-modified ADP analogs.
The Journal of biological chemistry
Blocking HIV entry.
Nature structural biology
Structural basis for selective inhibition of Src family kinases by PP1.
Chemistry & biology
Acquisition of inhibitor-sensitive protein kinases through protein design.
Pharmacology & therapeutics
Highly efficient green fluorescent protein-based kinase substrates.
Analytical biochemistry
A molecular gate which controls unnatural ATP analogue recognition by the tyrosine kinase v-Src.
Bioorganic & medicinal chemistry
Chromophore-assisted light inactivation and self-organization of microtubules and motors.
Proceedings of the National Academy of Sciences of the United States of America
Design of allele-specific inhibitors to probe protein kinase signaling.
Current biology : CB
Engineering Src family protein kinases with unnatural nucleotide specificity.
Chemistry & biology
Engineering unnatural nucleotide specificity for Rous sarcoma virus tyrosine kinase to uniquely label its direct substrates.
Proceedings of the National Academy of Sciences of the United States of America
Intravenous injection of soluble antigen induces thymic and peripheral T-cells apoptosis.
Proceedings of the National Academy of Sciences of the United States of America
Tyrosine kinases: modular signaling enzymes with tunable specificities.
Chemistry & biology
High-dose soluble antigen: peripheral T-cell proliferation or apoptosis.
Immunological reviews
Immunoglobulin signal transduction guides the specificity of B cell-T cell interactions and is blocked in tolerant self-reactive B cells.
The Journal of experimental medicine
Catalytic antibodies.
Methods in enzymology
The generation of antibody combining sites containing catalytic residues.
Ciba Foundation symposium
Catalytic antibodies.
Annual review of immunology