Kevan M Shokat

Kevan M Shokat

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Kevan M Shokat

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Bifunctional Small-Molecule Ligands of K-Ras Induce Its Association with Immunophilin Proteins.

Angew Chem Int Ed Engl 2019 Sep 26. Epub 2019 Sep 26.

Cellular and Molecular Pharmacology, Howard Hughes Medical Institute, University of California, San Francisco, 600 16th Street, San Francisco, CA, 94143, USA.

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http://dx.doi.org/10.1002/anie.201910124DOI Listing
September 2019

A Bounty of New Challenging Targets in Oncology for Chemical Discovery.

Biochemistry 2019 Aug 25;58(31):3328-3330. Epub 2019 Jul 25.

Department of Cellular and Molecular Pharmacology , University of California, San Francisco , San Francisco , California 94158 , United States.

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http://dx.doi.org/10.1021/acs.biochem.9b00570DOI Listing
August 2019

KRAS inhibition produces a driver-limited state revealing collateral dependencies.

Sci Signal 2019 May 28;12(583). Epub 2019 May 28.

Helen Diller Family Comprehensive Cancer Center, University of California, San Francisco, San Francisco, CA 94158, USA.

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http://dx.doi.org/10.1126/scisignal.aaw9450DOI Listing
May 2019

Chemically reprogramming the phospho-transfer reaction to crosslink protein kinases to their substrates.

Protein Sci 2019 Mar 31;28(3):654-662. Epub 2019 Jan 31.

Department of Cellular and Molecular Pharmacology, University of California San Francisco, San Francisco, California.

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http://doi.wiley.com/10.1002/pro.3570
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http://dx.doi.org/10.1002/pro.3570DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6371225PMC
March 2019

A Legionella pneumophila Kinase Phosphorylates the Hsp70 Chaperone Family to Inhibit Eukaryotic Protein Synthesis.

Cell Host Microbe 2019 03 28;25(3):454-462.e6. Epub 2019 Feb 28.

Department of Microbiology and Immunology, University of California, San Francisco, San Francisco, CA 94143, USA; George Williams Hooper Foundation, University of California, San Francisco, San Francisco, CA 94143, USA. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S19313128193004
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http://dx.doi.org/10.1016/j.chom.2019.01.006DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6529236PMC
March 2019

Chronic TGF-β exposure drives stabilized EMT, tumor stemness, and cancer drug resistance with vulnerability to bitopic mTOR inhibition.

Sci Signal 2019 Feb 26;12(570). Epub 2019 Feb 26.

Department of Cell and Tissue Biology, University of California at San Francisco, San Francisco, CA 94143, USA.

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http://dx.doi.org/10.1126/scisignal.aau8544DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6746178PMC
February 2019

Type II Kinase Inhibitors Targeting Cys-Gatekeeper Kinases Display Orthogonality with Wild Type and Ala/Gly-Gatekeeper Kinases.

ACS Chem Biol 2018 10 9;13(10):2956-2965. Epub 2018 Oct 9.

School of Molecular and Cellular Biology, Faculty of Biological Sciences , University of Leeds , Leeds LS2 9JT , U.K.

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http://dx.doi.org/10.1021/acschembio.8b00592DOI Listing
October 2018

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

Nucleic Acids Res 2018 09;46(17):8689-8699

Department of Cellular and Molecular Pharmacology, University of California, San Francisco, CA 94158, USA.

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http://dx.doi.org/10.1093/nar/gky706DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6158709PMC
September 2018

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

Nat Chem Biol 2018 08 25;14(8):768-777. Epub 2018 Jun 25.

Department of Bioengineering and Therapeutic Sciences, University of California San Francisco, San Francisco, CA, USA.

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http://dx.doi.org/10.1038/s41589-018-0081-9DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6051919PMC
August 2018

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

J Vis Exp 2018 08 28(138). Epub 2018 Aug 28.

Department of Cellular and Molecular Pharmacology and Howard Hughes Medical Institute, University of California San Francisco.

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https://www.jove.com/video/58265/a-high-throughput-luciferas
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http://dx.doi.org/10.3791/58265DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6231911PMC
August 2018

Disease-Causing Mutations in the G Protein Gαs Subvert the Roles of GDP and GTP.

Cell 2018 05 5;173(5):1254-1264.e11. Epub 2018 Apr 5.

Department of Cellular and Molecular Pharmacology and Howard Hughes Medical Institute, University of California-San Francisco, San Francisco, CA 94158, USA; Department of Chemistry, University of California-Berkeley, Berkeley, CA 94720, USA. Electronic address:

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http://dx.doi.org/10.1016/j.cell.2018.03.018DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5959768PMC
May 2018

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

Addict Biol 2018 03 6;23(2):713-722. Epub 2017 Jul 6.

Department of Neurology, University of California, San Francisco, CA, USA.

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http://dx.doi.org/10.1111/adb.12528DOI Listing
March 2018

Stepwise processing analyses of the single-turnover PCSK9 protease reveal its substrate sequence specificity and link clinical genotype to lipid phenotype.

J Biol Chem 2018 02 19;293(6):1875-1886. Epub 2017 Dec 19.

the Department of Cellular and Molecular Pharmacology and Howard Hughes Medical Institute, University of California, San Francisco, California 94143.

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http://dx.doi.org/10.1074/jbc.RA117.000754DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5808750PMC
February 2018

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

J Chem Inf Model 2018 02 31;58(2):464-471. Epub 2018 Jan 31.

Department of Organic Chemistry, The Weizmann Institute of Science , Rehovot, 7610001, Israel.

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http://dx.doi.org/10.1021/acs.jcim.7b00399DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6179444PMC
February 2018

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

Cell Chem Biol 2017 12 12;24(12):1455-1466.e14. Epub 2017 Oct 12.

Department of Cellular and Molecular Pharmacology, Howard Hughes Medical Institute, University of California, San Francisco, CA 94158, USA. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S24519456173032
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http://dx.doi.org/10.1016/j.chembiol.2017.08.025DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5915340PMC
December 2017

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

Neurochem Int 2017 Oct 20;109:106-116. Epub 2017 Apr 20.

Gladstone Institute of Neurological Disease, Gladstone Institutes, San Francisco, CA, USA; Department of Neurology, University of California, San Francisco, San Francisco, CA, USA. Electronic address:

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http://dx.doi.org/10.1016/j.neuint.2017.04.006DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5641232PMC
October 2017

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

Nat Chem Biol 2017 Aug 12;13(8):842-844. Epub 2017 Jun 12.

Department of Pharmaceutical Chemistry, University of California, San Francisco, San Francisco, California, USA.

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http://www.nature.com/doifinder/10.1038/nchembio.2406
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http://dx.doi.org/10.1038/nchembio.2406DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5577362PMC
August 2017

Drugging the 'undruggable' cancer targets.

Nat Rev Cancer 2017 08 23;17(8):502-508. Epub 2017 Jun 23.

Vall d'Hebron Institute of Oncology (VHIO), Cellex Centre, Barcelona 08035; Institució Catalana de Recerca i Estudis Avançats (ICREA), Barcelona 08010; and Department of Biochemistry and Molecular Biology, Universitat Autònoma de Barcelona, 08193 Bellaterra, Spain.

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http://dx.doi.org/10.1038/nrc.2017.36DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5945194PMC
August 2017

Farnesyltransferase-Mediated Delivery of a Covalent Inhibitor Overcomes Alternative Prenylation to Mislocalize K-Ras.

ACS Chem Biol 2017 07 19;12(7):1956-1962. Epub 2017 Jun 19.

Howard Hughes Medical Institute and Department of Cellular and Molecular Pharmacology, University of California San Francisco , San Francisco, California 94158, United States.

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http://dx.doi.org/10.1021/acschembio.7b00374DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6070134PMC
July 2017

INPP4B and PTEN Loss Leads to PI-3,4-P2 Accumulation and Inhibition of PI3K in TNBC.

Mol Cancer Res 2017 06 14;15(6):765-775. Epub 2017 Feb 14.

Department of Cellular and Molecular Pharmacology, University of California, San Francisco, California.

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http://dx.doi.org/10.1158/1541-7786.MCR-16-0183DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5502826PMC
June 2017

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

Biochemistry 2017 06 16;56(25):3178-3183. Epub 2017 Jun 16.

Howard Hughes Medical Institute and Department of Cellular and Molecular Pharmacology, University of California, San Francisco , San Francisco, California 94158, United States.

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http://dx.doi.org/10.1021/acs.biochem.7b00271DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5665167PMC
June 2017

A Kinase Inhibitor Targeted to mTORC1 Drives Regression in Glioblastoma.

Cancer Cell 2017 03;31(3):424-435

Department of Neurology, University of California, San Francisco, CA 94158, USA; Helen Diller Family Comprehensive Cancer Center, San Francisco, CA 94158, USA; Department of Pediatrics, University of California, San Francisco, CA 94158, USA; Department of Neurological Surgery, University of California, San Francisco, CA 94158, USA. Electronic address:

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http://dx.doi.org/10.1016/j.ccell.2017.01.014DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5386178PMC
March 2017

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

Antioxid Redox Signal 2017 01 5;26(2):70-83. Epub 2016 Aug 5.

1 Department of Biochemistry and Molecular Biology, School of Medicine, Kyung Hee University , Seoul, Republic of Korea.

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http://dx.doi.org/10.1089/ars.2015.6457DOI Listing
January 2017

Discovery of new substrates of the elongation factor-2 kinase suggests a broader role in the cellular nutrient response.

Cell Signal 2017 01 17;29:78-83. Epub 2016 Oct 17.

Howard Hughes Medical Institute and Department of Cellular and Molecular Pharmacology, University of California, San Francisco, San Francisco, CA 94158, USA. Electronic address:

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http://dx.doi.org/10.1016/j.cellsig.2016.10.006DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5138099PMC
January 2017

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

Mol Pharmacol 2017 Jan 7;91(1):65-73. Epub 2016 Nov 7.

Department of Psychiatry (Y.U., D.J., and M.Z.), Department of Cellular and Molecular Pharmacology (F.U.R., K.M.S., and M.Z.), and Howard Hughes Medical Institute (F.U.R. and K.M.S.), University of California, San Francisco, San Francisco, California

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http://dx.doi.org/10.1124/mol.116.106252DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5198513PMC
January 2017

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

Nat Chem Biol 2016 Nov 5;12(11):923-930. Epub 2016 Sep 5.

Howard Hughes Medical Institute, University of California San Francisco, San Francisco, California, USA.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5069157PMC
http://dx.doi.org/10.1038/nchembio.2171DOI Listing
November 2016

Direct small-molecule inhibitors of KRAS: from structural insights to mechanism-based design.

Nat Rev Drug Discov 2016 11 29;15(11):771-785. Epub 2016 Jul 29.

Department of Cellular and Molecular Pharmacology, Howard Hughes Medical Institute, University of California, San Francisco, California 94143, USA.

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http://dx.doi.org/10.1038/nrd.2016.139DOI Listing
November 2016

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

Proc Natl Acad Sci U S A 2016 08 1;113(33):E4776-83. Epub 2016 Aug 1.

Department of Microbiology and Immunology, University of California, San Francisco, CA 94143

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http://dx.doi.org/10.1073/pnas.1608355113DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4995946PMC
August 2016

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

Mol Cancer Ther 2016 07 30;15(7):1472-84. Epub 2016 Jun 30.

The CRUK Gene Function Laboratory, The Institute of Cancer Research, London, United Kingdom. Breakthrough Breast Cancer Research Centre, The Institute of Cancer Research, London, United Kingdom.

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http://dx.doi.org/10.1158/1535-7163.MCT-15-0554DOI Listing
July 2016

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

Nature 2016 06 18;534(7606):272-6. Epub 2016 May 18.

Howard Hughes Medical Institute and Department of Cellular and Molecular Pharmacology, University of California San Francisco, San Francisco, California 94158, USA.

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http://www.nature.com/articles/nature17963
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http://dx.doi.org/10.1038/nature17963DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4902179PMC
June 2016

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

Anal Chem 2016 05 28;88(10):5042-5. Epub 2016 Apr 28.

School of Materials Science and Engineering and Centre for Biomimetic Sensor Science, Nanyang Technological University , 50 Nanyang Avenue, 639798, Singapore.

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http://dx.doi.org/10.1021/acs.analchem.6b01293DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5291064PMC
May 2016

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

Cancer Cell 2016 Apr 31;29(4):536-547. Epub 2016 Mar 31.

Department of Microbiology, Immunology, and Medical Genetics, University of California, Los Angeles, Los Angeles, CA 90095, USA; Eli and Edythe Broad Center of Regenerative Medicine and Stem Cell Research, University of California, Los Angeles, Los Angeles, CA 90095, USA; Department of Molecular and Medical Pharmacology, University of California, Los Angeles, Los Angeles, CA 90095, USA; Howard Hughes Medical Institute, University of California, Los Angeles, Los Angeles, CA 90095, USA. Electronic address:

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http://dx.doi.org/10.1016/j.ccell.2016.03.001DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4829466PMC
April 2016

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

Protein Sci 2016 Mar 26;25(3):638-49. Epub 2015 Dec 26.

Department of Molecular and Cell Biology, University of California, Berkeley, California.

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http://dx.doi.org/10.1002/pro.2857DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4815421PMC
March 2016

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

Cell Metab 2015 Nov 8;22(5):907-21. Epub 2015 Oct 8.

Cancer Biology Program, Stanford University, Stanford, CA 94305, USA; Department of Genetics, Stanford University, Stanford, CA 94305, USA; Glenn Laboratories for the Biology of Aging, Stanford, CA 94305, USA. Electronic address:

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http://www.cell.com/cell-metabolism/pdf/S1550-4131(15)00466-
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http://linkinghub.elsevier.com/retrieve/pii/S155041311500466
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http://dx.doi.org/10.1016/j.cmet.2015.09.009DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4635044PMC
November 2015

Discovery and structure of a new inhibitor scaffold of the autophagy initiating kinase ULK1.

Bioorg Med Chem 2015 Sep 26;23(17):5483-8. Epub 2015 Jul 26.

Howard Hughes Medical Institute and Department of Cellular and Molecular Pharmacology, University of California, San Francisco, San Francisco, CA 94158, USA. Electronic address:

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http://dx.doi.org/10.1016/j.bmc.2015.07.034DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4864979PMC
September 2015

SR protein kinases promote splicing of nonconsensus introns.

Nat Struct Mol Biol 2015 Aug 13;22(8):611-7. Epub 2015 Jul 13.

Department of Biochemistry and Biophysics, University of California, San Francisco, San Francisco, California, USA.

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http://dx.doi.org/10.1038/nsmb.3057DOI Listing
August 2015

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

Elife 2015 Aug 24;4. Epub 2015 Aug 24.

Rosalind Russell and Ephraim P. Engleman Rheumatology Research Center, Division of Rheumatology, Department of Medicine, University of California, San Francisco, San Francisco, United States.

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http://dx.doi.org/10.7554/eLife.08088DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4568592PMC
August 2015

The logic and design of analog-sensitive kinases and their small molecule inhibitors.

Methods Enzymol 2014 ;548:189-213

Howard Hughes Medical Institute and Department of Cellular & Molecular Pharmacology, University of California, San Francisco, California, USA.

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http://dx.doi.org/10.1016/B978-0-12-397918-6.00008-2DOI Listing
July 2015

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

Sci Signal 2015 Jun 30;8(383):ra65. Epub 2015 Jun 30.

Institut de Neurobiologie de la Méditerranée (INMED), INSERM Unité 901, 13273 Marseille, France. Aix-Marseille Université, UMR 901, 13273 Marseille, France.

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http://dx.doi.org/10.1126/scisignal.aaa0354DOI Listing
June 2015

Differential genetic interactions of yeast stress response MAPK pathways.

Mol Syst Biol 2015 Apr 17;11(4):800. Epub 2015 Apr 17.

Department of Cellular and Molecular Pharmacology, University of California, San Francisco, CA USA Center for Systems and Synthetic Biology, University of California, San Francisco, CA, USA California Institute for Quantitative Biosciences, QB3, San Francisco, CA, USA J. David Gladstone Institutes, San Francisco, CA, USA

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http://msb.embopress.org/cgi/doi/10.15252/msb.20145606
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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4422557PMC
http://dx.doi.org/10.15252/msb.20145606DOI Listing
April 2015

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

Mol Cancer Ther 2015 Feb 18;14(2):419-28. Epub 2014 Dec 18.

Department of Neurology, University of California, San Francisco, California. Department of Neurological Surgery and Brain Tumor Research Center, University of California, San Francisco, California. Sandler Neurosciences Center, University of California, San Francisco, California.

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http://dx.doi.org/10.1158/1535-7163.MCT-14-0526DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4326592PMC
February 2015

Structure of the human autophagy initiating kinase ULK1 in complex with potent inhibitors.

ACS Chem Biol 2015 Jan 6;10(1):257-61. Epub 2015 Jan 6.

Howard Hughes Medical Institute and Department of Cellular and Molecular Pharmacology, University of California, San Francisco , San Francisco, California 94158, United States.

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http://dx.doi.org/10.1021/cb500835zDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4301081PMC
January 2015

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

Neuron 2014 Dec 13;84(5):968-82. Epub 2014 Nov 13.

Departments of Physiology, Biochemistry, and Biophysics, University of California, San Francisco, San Francisco, CA 94158, USA; Howard Hughes Medical Institute, University of California, San Francisco, San Francisco, CA 94158, USA. Electronic address:

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http://dx.doi.org/10.1016/j.neuron.2014.10.025DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4407996PMC
December 2014

Targeting osteosarcoma.

Proc Natl Acad Sci U S A 2014 Dec 15;111(51):18100-1. Epub 2014 Dec 15.

Department of Cellular and Molecular Pharmacology and Howard Hughes Medical Institute, University of California, San Francisco, CA 94158

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http://dx.doi.org/10.1073/pnas.1420596111DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4280583PMC
December 2014

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

Elife 2014 Dec 22;3. Epub 2014 Dec 22.

Department of Cellular and Molecular Pharmacology, Howard Hughes Medical Institute, University of California, San Francisco, San Francisco, United States.

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https://elifesciences.org/articles/03445
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http://dx.doi.org/10.7554/eLife.03445DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4307180PMC
December 2014

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

J Appl Physiol (1985) 2014 Oct 28;117(8):910-20. Epub 2014 Aug 28.

Department of Physiology and Biomedical Engineering, Mayo Clinic College of Medicine, Rochester, Minnesota; Department of Anesthesiology, Mayo Clinic College of Medicine, Rochester, Minnesota; and.

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http://jap.physiology.org/content/jap/117/8/910.full.pdf
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http://jap.physiology.org/content/jap/early/2014/08/25/jappl
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http://jap.physiology.org/cgi/doi/10.1152/japplphysiol.01386
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http://dx.doi.org/10.1152/japplphysiol.01386.2013DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4199990PMC
October 2014

The proprotein convertase subtilisin/kexin type 9 (PCSK9) active site and cleavage sequence differentially regulate protein secretion from proteolysis.

J Biol Chem 2014 Oct 10;289(42):29030-43. Epub 2014 Sep 10.

Cardiovascular Research Institute, University of California, San Francisco, California 94158, and Department of Cellular and Molecular Pharmacology, University of California, San Francisco, California 94158 and Department of Chemistry, University of California, Berkeley, California 94720.

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http://dx.doi.org/10.1074/jbc.M114.594861DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4200258PMC
October 2014

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

Proc Natl Acad Sci U S A 2014 Sep 18;111(35):E3679-88. Epub 2014 Aug 18.

Rosalind Russell and Ephraim P. Engleman Arthritis Research Center, Division of Rheumatology, Department of Medicine, Howard Hughes Medical Institute, University of California, San Francisco, CA 94143

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http://www.pnas.org/content/111/35/E3679.full.pdf
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http://www.pnas.org/cgi/doi/10.1073/pnas.1413726111
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http://dx.doi.org/10.1073/pnas.1413726111DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4156735PMC
September 2014

Drugging MYCN through an allosteric transition in Aurora kinase A.

Cancer Cell 2014 Sep 28;26(3):414-427. Epub 2014 Aug 28.

Department of Pediatrics, UCSF Benioff Children's Hospital, University of California, San Francisco, San Francisco, CA 94158, USA; Departments of Neurology and Neurological Surgery, University of California, San Francisco, San Francisco, CA 94158, USA; Helen Diller Family Comprehensive Cancer Center, University of California, San Francisco, San Francisco, CA 94158, USA. Electronic address:

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http://dx.doi.org/10.1016/j.ccr.2014.07.015DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4160413PMC
September 2014

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

Cell Rep 2014 Aug 7;8(4):1037-48. Epub 2014 Aug 7.

Howard Hughes Medical Institute and Department of Cellular and Molecular Pharmacology, University of California, San Francisco, San Francisco, CA 94158, USA. Electronic address:

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http://dx.doi.org/10.1016/j.celrep.2014.07.010DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4294625PMC
August 2014

Adipocyte ALK7 links nutrient overload to catecholamine resistance in obesity.

Elife 2014 Aug 25;3:e03245. Epub 2014 Aug 25.

Department of Neuroscience, Karolinska Institutet, Stockholm, Sweden Department of Physiology, National University of Singapore, Singapore, Singapore Life Sciences Institute, National University of Singapore, Singapore, Singapore

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4139062PMC
http://dx.doi.org/10.7554/eLife.03245DOI Listing
August 2014

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

Nat Immunol 2014 Jul 8;15(7):687-94. Epub 2014 Jun 8.

1] Howard Hughes Medical Institute, University of California, San Francisco, San Francisco, California, USA. [2] Rosalind Russell-Ephraim P. Engleman Rheumatology Research Center, University of California, San Francisco, San Francisco, California, USA. [3] Department of Medicine, University of California, San Francisco, San Francisco, California, USA. [4] Department of Microbiology and Immunology, University of California, San Francisco, San Francisco, California, USA.

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http://dx.doi.org/10.1038/ni.2918DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4095875PMC
July 2014

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

Proc Natl Acad Sci U S A 2014 Jul 24;111(27):9983-8. Epub 2014 Jun 24.

Department of Bioengineering and Therapeutic Sciences, Schools of Pharmacy and Medicine, University of California, San Francisco, CA 94143-2911;Institute for Human Genetics, University of California, San Francisco, CA 94143

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http://dx.doi.org/10.1073/pnas.1314939111DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4103324PMC
July 2014

A crosslinker based on a tethered electrophile for mapping kinase-substrate networks.

Chem Biol 2014 May 17;21(5):585-90. Epub 2014 Apr 17.

Chemistry and Chemical Biology Graduate Program, University of California, San Francisco, 600 16(th) Street, MC2280, San Francisco, CA 94158, USA. Electronic address:

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http://dx.doi.org/10.1016/j.chembiol.2014.02.022DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4627693PMC
May 2014

Inhibition of the kinase Csk in thymocytes reveals a requirement for actin remodeling in the initiation of full TCR signaling.

Nat Immunol 2014 Feb 8;15(2):186-94. Epub 2013 Dec 8.

1] Rosalind Russell-Ephraim P. Engleman Medical Research Center for Arthritis, Division of Rheumatology, Department of Medicine, University of California, San Francisco, California, USA. [2] Howard Hughes Medical Institute, Chevy Chase, Maryland, USA. [3] Department of Microbiology and Immunology, University of California, San Francisco, California, USA.

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http://www.nature.com/articles/ni.2772
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http://dx.doi.org/10.1038/ni.2772DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3946925PMC
February 2014

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

J Am Chem Soc 2013 Dec 20;135(48):18153-9. Epub 2013 Nov 20.

Howard Hughes Medical Institute and Department of Cellular & Molecular Pharmacology, University of California , San Francisco, California 94143, United States.

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http://dx.doi.org/10.1021/ja408704uDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3938282PMC
December 2013

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

Cell Rep 2013 Dec 19;5(6):1725-36. Epub 2013 Dec 19.

Department of Cellular and Molecular Pharmacology, University of California, San Francisco, San Francisco, CA 94158, USA; California Institute for Quantitative Biosciences, QB3, San Francisco, CA 94158, USA; Howard Hughes Medical Institute, San Francisco, CA 94158, USA. Electronic address:

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http://dx.doi.org/10.1016/j.celrep.2013.11.040DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4007695PMC
December 2013

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

Nature 2013 Nov 20;503(7477):548-51. Epub 2013 Nov 20.

1] Department of Cellular and Molecular Pharmacology, Howard Hughes Medical Institute, University of California, San Francisco, California 94158, USA [2].

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http://www.nature.com/articles/nature12796
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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4274051PMC
November 2013

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

Cancer Cell 2013 Oct;24(4):438-49

Department of Neurology, University of California, San Francisco, 1450 Third Street, MC0520, San Francisco, CA 94158-9001, USA; Helen Diller Family Comprehensive Cancer Center, University of California, San Francisco, 1450 Third Street, MC0520, San Francisco, CA 94158-9001, USA. Electronic address:

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http://dx.doi.org/10.1016/j.ccr.2013.09.004DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3819146PMC
October 2013

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

ACS Chem Biol 2013 Sep 23;8(9):1931-8. Epub 2013 Jul 23.

Howard Hughes Medical Institute and Department of Cellular & Molecular Pharmacology, University of California, San Francisco , San Francisco, California 94158, United States.

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http://dx.doi.org/10.1021/cb400376pDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3938192PMC
September 2013

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

Cell 2013 Aug;154(4):737-47

Howard Hughes Medical Institute and Department of Cellular and Molecular Pharmacology, University of California, San Francisco, San Francisco, CA 94158, USA.

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http://dx.doi.org/10.1016/j.cell.2013.07.030DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3950538PMC
August 2013

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

Cancer Med 2013 Aug 10;2(4):496-506. Epub 2013 Jun 10.

Department of Internal Medicine Division of Hematology/Oncology Helen Diller Family Comprehensive Cancer Center, University of California San Francisco, California, USA.

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http://dx.doi.org/10.1002/cam4.97DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3799284PMC
August 2013

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

Proc Natl Acad Sci U S A 2013 Jul 26;110(29):11988-93. Epub 2013 Jun 26.

School of Medicine and Department of Urology, Helen Diller Family Comprehensive Cancer Center, University of California, San Francisco, CA 94158, USA.

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http://dx.doi.org/10.1073/pnas.1310230110DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3718086PMC
July 2013

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

J Med Chem 2013 Apr 26;56(7):3068-77. Epub 2013 Mar 26.

Department of Molecular Microbiology, Washington University School of Medicine, 660 South Euclid Avenue, St Louis Missouri 63110, United States.

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http://dx.doi.org/10.1021/jm4001314DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3625458PMC
April 2013

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

Mol Cell 2013 Apr;50(2):250-60

Department of Structural and Chemical Biology, Graduate School of Biomedical Sciences, Icahn School of Medicine at Mount Sinai, New York, NY 10029-6574, USA.

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http://dx.doi.org/10.1016/j.molcel.2013.04.003DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3677717PMC
April 2013

A method to site-specifically incorporate methyl-lysine analogues into recombinant proteins.

Methods Enzymol 2012 ;512:57-69

Department of Molecular Biophysics and Biochemistry, Chemical Biology Institute, Yale University, New Haven, Connecticut, USA.

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http://dx.doi.org/10.1016/B978-0-12-391940-3.00003-2DOI Listing
December 2012

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

Nat Struct Mol Biol 2012 Nov 14;19(11):1108-15. Epub 2012 Oct 14.

Department of Structural and Chemical Biology, Mount Sinai School of Medicine, New York, New York, USA.

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http://dx.doi.org/10.1038/nsmb.2399DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3746743PMC
November 2012

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

Cancer Res 2012 Aug 19;72(16):4214-24. Epub 2012 Jun 19.

Department of Biochemistry and Molecular Biology (BK21 project), Medical Research Center for Bioreaction to Reactive Oxygen Species and Biomedical Science Institute, School of Medicine, Kyung Hee University, Seoul, Republic of Korea.

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http://dx.doi.org/10.1158/0008-5472.CAN-12-1110DOI Listing
August 2012

Chemical genetic discovery of targets and anti-targets for cancer polypharmacology.

Nature 2012 Jun 6;486(7401):80-4. Epub 2012 Jun 6.

Howard Hughes Medical Institute and Department of Cellular and Molecular Pharmacology, University of California, San Francisco, California 94158, USA.

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http://www.nature.com/articles/nature11127
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http://dx.doi.org/10.1038/nature11127DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3703503PMC
June 2012