Nathanael S Gray

Nathanael S Gray

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Nathanael S Gray

Publications by authors named "Nathanael S Gray"

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Synthetic Lethal Interaction of SHOC2 Depletion with MEK Inhibition in RAS-Driven Cancers.

Cell Rep 2019 Oct;29(1):118-134.e8

Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA; Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, MA 02215, USA; Harvard Medical School, 25 Shattuck Street, Boston, MA 02115, USA; Department of Medicine, Brigham and Women's Hospital and Harvard Medical School, 75 Francis Street, Boston, MA 02115, MA. Electronic address:

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http://dx.doi.org/10.1016/j.celrep.2019.08.090DOI Listing
October 2019

Dual Inhibition of TAF1 and BET Bromodomains from the BI-2536 Kinase Inhibitor Scaffold.

ACS Med Chem Lett 2019 Oct 13;10(10):1443-1449. Epub 2019 Sep 13.

Department of Cancer Biology, Dana Farber Cancer Institute, Boston Massachusetts 02115, United States.

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http://dx.doi.org/10.1021/acsmedchemlett.9b00243DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6792166PMC
October 2019

Synthesis and structure activity relationships of a series of 4-amino-1H-pyrazoles as covalent inhibitors of CDK14.

Bioorg Med Chem Lett 2019 Aug 23;29(15):1985-1993. Epub 2019 May 23.

Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02215, USA. Electronic address:

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http://dx.doi.org/10.1016/j.bmcl.2019.05.024DOI Listing
August 2019

JNK2 Is Required for the Tumorigenic Properties of Melanoma Cells.

ACS Chem Biol 2019 Jul 17;14(7):1426-1435. Epub 2019 May 17.

Department of Translational Molecular Pathology , The University of Texas M. D. Anderson Cancer Center , Houston , Texas 77030 , United States.

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http://dx.doi.org/10.1021/acschembio.9b00083DOI Listing
July 2019

Quinoline and thiazolopyridine allosteric inhibitors of MALT1.

Bioorg Med Chem Lett 2019 Jul 20;29(14):1694-1698. Epub 2019 May 20.

Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02115, USA; Department of Biological Chemistry & Molecular Pharmacology, Harvard Medical School, 360 Longwood Ave, Boston, MA 02115, USA.

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http://dx.doi.org/10.1016/j.bmcl.2019.05.040DOI Listing
July 2019

Development of a Selective CDK7 Covalent Inhibitor Reveals Predominant Cell-Cycle Phenotype.

Cell Chem Biol 2019 Jun 21;26(6):792-803.e10. Epub 2019 Mar 21.

Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02215, USA; Department of Biology Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02215, USA. Electronic address:

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http://dx.doi.org/10.1016/j.chembiol.2019.02.012DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6588464PMC
June 2019

Peptide-based covalent inhibitors of MALT1 paracaspase.

Bioorg Med Chem Lett 2019 Jun 29;29(11):1336-1339. Epub 2019 Mar 29.

Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02115, USA; Department of Biological Chemistry & Molecular Pharmacology, Harvard Medical School, 360 Longwood Ave, Boston, MA 02115, USA. Electronic address:

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http://dx.doi.org/10.1016/j.bmcl.2019.03.046DOI Listing
June 2019

Leveraging Compound Promiscuity to Identify Targetable Cysteines within the Kinome.

Cell Chem Biol 2019 Jun 11;26(6):818-829.e9. Epub 2019 Apr 11.

Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02115, USA; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02115, USA. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S24519456193007
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http://dx.doi.org/10.1016/j.chembiol.2019.02.021DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6634314PMC
June 2019

Development of Dual and Selective Degraders of Cyclin-Dependent Kinases 4 and 6.

Angew Chem Int Ed Engl 2019 May 29;58(19):6321-6326. Epub 2019 Mar 29.

Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA.

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http://dx.doi.org/10.1002/anie.201901336DOI Listing
May 2019

A multitargeted probe-based strategy to identify signaling vulnerabilities in cancers.

J Biol Chem 2019 May 11;294(21):8664-8673. Epub 2019 Mar 11.

Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, Massachusetts 02115

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http://www.jbc.org/lookup/doi/10.1074/jbc.RA118.006805
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http://dx.doi.org/10.1074/jbc.RA118.006805DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6544847PMC
May 2019

BCL2 Amplicon Loss and Transcriptional Remodeling Drives ABT-199 Resistance in B Cell Lymphoma Models.

Cancer Cell 2019 May;35(5):752-766.e9

Chemical Biology and Molecular Medicine Program, Moffitt Cancer Center & Research Institute, Tampa, FL 33612, USA; Department of Laboratory Medicine and Hematopathology, Moffitt Cancer Center & Research Institute, Tampa, FL 33612, USA. Electronic address:

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http://dx.doi.org/10.1016/j.ccell.2019.04.005DOI Listing
May 2019

Identification of small molecule inhibitors targeting the Zika virus envelope protein.

Antiviral Res 2019 Apr 13;164:147-153. Epub 2019 Feb 13.

Department of Microbiology and Blavatnik Institute, Harvard Medical School, 77 Avenue Louis Pasteur, Boston, MA 02115, USA. Electronic address:

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http://dx.doi.org/10.1016/j.antiviral.2019.02.008DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6675404PMC
April 2019

Small Molecules Targeting the Flavivirus E Protein with Broad-Spectrum Activity and Antiviral Efficacy in Vivo.

ACS Infect Dis 2019 Mar 14;5(3):460-472. Epub 2019 Jan 14.

Department of Microbiology, Blavatnik Institute , Harvard Medical School , 77 Avenue Louis Pasteur , Boston , Massachusetts 02115 , United States.

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http://dx.doi.org/10.1021/acsinfecdis.8b00322DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6548335PMC
March 2019

Conformational flexibility and inhibitor binding to unphosphorylated interleukin-1 receptor-associated kinase 4 (IRAK4).

J Biol Chem 2019 03 24;294(12):4511-4519. Epub 2019 Jan 24.

From the Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, Massachusetts 02115,

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http://www.jbc.org/lookup/doi/10.1074/jbc.RA118.005428
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http://dx.doi.org/10.1074/jbc.RA118.005428DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6433055PMC
March 2019

Specific covalent inhibition of MALT1 paracaspase suppresses B cell lymphoma growth.

J Clin Invest 2018 10 19;128(10):4397-4412. Epub 2018 Jul 19.

Division of Hematology and Oncology, Department of Medicine, Weill Cornell Medicine, Cornell University, New York, New York, USA.

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http://dx.doi.org/10.1172/JCI99436DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6159983PMC
October 2018

Targeting the Extracellular Signal-Regulated Kinase 5 Pathway to Suppress Human Chronic Myeloid Leukemia Stem Cells.

Stem Cell Reports 2018 10 20;11(4):929-943. Epub 2018 Sep 20.

Department of Experimental and Clinical Biomedical Sciences, Università degli Studi di Firenze, viale G.B. Morgagni, 50, Firenze 50134, Italy; Istituto Toscano Tumori (ITT), Firenze 50134, Italy. Electronic address:

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http://dx.doi.org/10.1016/j.stemcr.2018.08.016DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6178886PMC
October 2018

Small-Molecule Inhibitors of LRRK2.

Adv Neurobiol 2017 ;14:241-264

Department of Cancer Biology, Dana Farber Cancer Institute, 450 Brookline Ave, Boston, MA, 02215, USA.

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http://dx.doi.org/10.1007/978-3-319-49969-7_13DOI Listing
September 2018

BMX-Mediated Regulation of Multiple Tyrosine Kinases Contributes to Castration Resistance in Prostate Cancer.

Cancer Res 2018 09 16;78(18):5203-5215. Epub 2018 Jul 16.

Hematology-Oncology Division, Department of Medicine, and Cancer Center, Beth Israel Deaconess Medical Center, Boston, Massachusetts.

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http://dx.doi.org/10.1158/0008-5472.CAN-17-3615DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6139052PMC
September 2018

Discovery of Immunologically Inspired Small Molecules That Target the Viral Envelope Protein.

ACS Infect Dis 2018 09 29;4(9):1395-1406. Epub 2018 Aug 29.

Department of Microbiology and Immunobiology , Harvard Medical School , 77 Avenue Louis Pasteur , Boston , Massachusetts 02115 , United States.

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http://pubs.acs.org/doi/10.1021/acsinfecdis.8b00127
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http://dx.doi.org/10.1021/acsinfecdis.8b00127DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6392429PMC
September 2018

Novel Scaffolds for Dual Specificity Tyrosine-Phosphorylation-Regulated Kinase (DYRK1A) Inhibitors.

J Med Chem 2018 09 23;61(17):7560-7572. Epub 2018 Aug 23.

The Norwegian Structural Biology Centre, Department of Chemistry , UiT The Arctic University of Norway , N-9037 Tromsø , Norway.

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http://dx.doi.org/10.1021/acs.jmedchem.7b01847DOI Listing
September 2018

First SAR Study for Overriding NRAS Mutant Driven Acute Myeloid Leukemia.

J Med Chem 2018 09 11;61(18):8353-8373. Epub 2018 Sep 11.

KU-KIST Graduate School of Converging Science and Technology , Korea University , 145 Anam-ro, Seongbuk-gu , Seoul 02841 , Republic of Korea.

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http://pubs.acs.org/doi/10.1021/acs.jmedchem.8b00882
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http://dx.doi.org/10.1021/acs.jmedchem.8b00882DOI Listing
September 2018

High MITF Expression Is Associated with Super-Enhancers and Suppressed by CDK7 Inhibition in Melanoma.

J Invest Dermatol 2018 07 8;138(7):1582-1590. Epub 2018 Feb 8.

Wellman Center for Photomedicine and Department of Dermatology, Massachusetts General Hospital, Harvard Medical School, Boston, Massachusetts, USA. Electronic address:

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http://dx.doi.org/10.1016/j.jid.2017.09.056DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6019629PMC
July 2018

How small-molecule inhibitors of dengue-virus infection interfere with viral membrane fusion.

Elife 2018 07 12;7. Epub 2018 Jul 12.

Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, United States.

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http://dx.doi.org/10.7554/eLife.36461DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6056230PMC
July 2018

Structure of the Human cGAS-DNA Complex Reveals Enhanced Control of Immune Surveillance.

Cell 2018 07;174(2):300-311.e11

Department of Microbiology and Immunobiology, Harvard Medical School, Boston, MA 02115, USA; Department of Cancer Immunology and Virology, Dana-Farber Cancer Institute, Boston, MA 02115, USA. Electronic address:

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http://dx.doi.org/10.1016/j.cell.2018.06.026DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6084792PMC
July 2018

Selective Inhibition of the Myeloid Src-Family Kinase Fgr Potently Suppresses AML Cell Growth in Vitro and in Vivo.

ACS Chem Biol 2018 06 30;13(6):1551-1559. Epub 2018 May 30.

Department of Microbiology and Molecular Genetics , University of Pittsburgh School of Medicine , Pittsburgh , Pennsylvania , United States.

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http://pubs.acs.org/doi/10.1021/acschembio.8b00154
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http://dx.doi.org/10.1021/acschembio.8b00154DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6130198PMC
June 2018

Development of Highly Potent and Selective Steroidal Inhibitors and Degraders of CDK8.

ACS Med Chem Lett 2018 Jun 18;9(6):540-545. Epub 2018 Mar 18.

Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, Massachusetts 02115, United States.

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https://pubs.acs.org/doi/10.1021/acsmedchemlett.8b00011
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http://dx.doi.org/10.1021/acsmedchemlett.8b00011DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6004574PMC
June 2018

ERK5 is activated by oncogenic BRAF and promotes melanoma growth.

Oncogene 2018 05 27;37(19):2601-2614. Epub 2018 Feb 27.

Department of Clinical and Experimental Biomedical Sciences, University of Florence, Florence, Italy.

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http://dx.doi.org/10.1038/s41388-018-0164-9DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5945581PMC
May 2018

Kinase inhibitors: the road ahead.

Nat Rev Drug Discov 2018 05 16;17(5):353-377. Epub 2018 Mar 16.

Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, United States.

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http://dx.doi.org/10.1038/nrd.2018.21DOI Listing
May 2018

Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK).

J Med Chem 2018 05 24;61(9):4249-4255. Epub 2018 Apr 24.

Department of Biological Chemistry & Molecular Pharmacology , Harvard Medical School , Boston , Massachusetts 02115 , United States.

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http://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01655
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http://dx.doi.org/10.1021/acs.jmedchem.7b01655DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6294449PMC
May 2018

SRPKIN-1: A Covalent SRPK1/2 Inhibitor that Potently Converts VEGF from Pro-angiogenic to Anti-angiogenic Isoform.

Cell Chem Biol 2018 04 22;25(4):460-470.e6. Epub 2018 Feb 22.

Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02115, USA; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02115, USA. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S24519456183003
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http://dx.doi.org/10.1016/j.chembiol.2018.01.013DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5973797PMC
April 2018

It Takes Two To Target: A Study in KRAS Dimerization.

Biochemistry 2018 04 12;57(16):2289-2290. Epub 2018 Apr 12.

Department of Cancer Biology , Dana-Farber Cancer Institute , Boston , Massachusetts 02215 , United States.

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http://dx.doi.org/10.1021/acs.biochem.8b00376DOI Listing
April 2018

Myeloid ERK5 deficiency suppresses tumor growth by blocking protumor macrophage polarization via STAT3 inhibition.

Proc Natl Acad Sci U S A 2018 03 5;115(12):E2801-E2810. Epub 2018 Mar 5.

Division of Cancer Sciences, School of Medical Sciences, Faculty of Biology, Medicine and Health, University of Manchester, Manchester M13 9PT, United Kingdom;

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http://www.pnas.org/lookup/doi/10.1073/pnas.1707929115
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http://dx.doi.org/10.1073/pnas.1707929115DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5866536PMC
March 2018

Overcoming Resistance to the THZ Series of Covalent Transcriptional CDK Inhibitors.

Cell Chem Biol 2018 02 21;25(2):135-142.e5. Epub 2017 Dec 21.

Department of Pediatric Oncology, Dana-Farber Cancer Institute, Boston, MA 02115, USA; Department of Pediatrics, Harvard Medical School, Boston, MA 02115, USA. Electronic address:

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http://dx.doi.org/10.1016/j.chembiol.2017.11.007DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6389506PMC
February 2018

EWS/FLI Confers Tumor Cell Synthetic Lethality to CDK12 Inhibition in Ewing Sarcoma.

Cancer Cell 2018 02 18;33(2):202-216.e6. Epub 2018 Jan 18.

Department of Pediatric Oncology, Dana-Farber Cancer Institute and Boston Children's Hospital, Harvard Medical School, 450 Brookline Avenue, Boston, MA 02215, USA; The Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S15356108173056
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http://dx.doi.org/10.1016/j.ccell.2017.12.009DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5846483PMC
February 2018

A Chemoproteomic Approach to Query the Degradable Kinome Using a Multi-kinase Degrader.

Cell Chem Biol 2018 01 9;25(1):88-99.e6. Epub 2017 Nov 9.

Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02115, USA; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02115, USA. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S24519456173038
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http://dx.doi.org/10.1016/j.chembiol.2017.10.005DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6427047PMC
January 2018

The Library of Integrated Network-Based Cellular Signatures NIH Program: System-Level Cataloging of Human Cells Response to Perturbations.

Authors:
Alexandra B Keenan Sherry L Jenkins Kathleen M Jagodnik Simon Koplev Edward He Denis Torre Zichen Wang Anders B Dohlman Moshe C Silverstein Alexander Lachmann Maxim V Kuleshov Avi Ma'ayan Vasileios Stathias Raymond Terryn Daniel Cooper Michele Forlin Amar Koleti Dusica Vidovic Caty Chung Stephan C Schürer Jouzas Vasiliauskas Marcin Pilarczyk Behrouz Shamsaei Mehdi Fazel Yan Ren Wen Niu Nicholas A Clark Shana White Naim Mahi Lixia Zhang Michal Kouril John F Reichard Siva Sivaganesan Mario Medvedovic Jaroslaw Meller Rick J Koch Marc R Birtwistle Ravi Iyengar Eric A Sobie Evren U Azeloglu Julia Kaye Jeannette Osterloh Kelly Haston Jaslin Kalra Steve Finkbiener Jonathan Li Pamela Milani Miriam Adam Renan Escalante-Chong Karen Sachs Alex Lenail Divya Ramamoorthy Ernest Fraenkel Gavin Daigle Uzma Hussain Alyssa Coye Jeffrey Rothstein Dhruv Sareen Loren Ornelas Maria Banuelos Berhan Mandefro Ritchie Ho Clive N Svendsen Ryan G Lim Jennifer Stocksdale Malcolm S Casale Terri G Thompson Jie Wu Leslie M Thompson Victoria Dardov Vidya Venkatraman Andrea Matlock Jennifer E Van Eyk Jacob D Jaffe Malvina Papanastasiou Aravind Subramanian Todd R Golub Sean D Erickson Mohammad Fallahi-Sichani Marc Hafner Nathanael S Gray Jia-Ren Lin Caitlin E Mills Jeremy L Muhlich Mario Niepel Caroline E Shamu Elizabeth H Williams David Wrobel Peter K Sorger Laura M Heiser Joe W Gray James E Korkola Gordon B Mills Mark LaBarge Heidi S Feiler Mark A Dane Elmar Bucher Michel Nederlof Damir Sudar Sean Gross David F Kilburn Rebecca Smith Kaylyn Devlin Ron Margolis Leslie Derr Albert Lee Ajay Pillai

Cell Syst 2018 01 29;6(1):13-24. Epub 2017 Nov 29.

NIH, Bethesda, MD 20892, USA.

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http://dx.doi.org/10.1016/j.cels.2017.11.001DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5799026PMC
January 2018

Crystal structure of human IRAK1.

Proc Natl Acad Sci U S A 2017 12 5;114(51):13507-13512. Epub 2017 Dec 5.

Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02115;

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http://dx.doi.org/10.1073/pnas.1714386114DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5754798PMC
December 2017

YY1 Is a Structural Regulator of Enhancer-Promoter Loops.

Cell 2017 Dec 7;171(7):1573-1588.e28. Epub 2017 Dec 7.

Whitehead Institute for Biomedical Research, Cambridge, MA 02142, USA; Department of Biology, Massachusetts Institute of Technology, Cambridge, MA 02142, USA. Electronic address:

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http://dx.doi.org/10.1016/j.cell.2017.11.008DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5785279PMC
December 2017

Dual inhibition of Fes and Flt3 tyrosine kinases potently inhibits Flt3-ITD+ AML cell growth.

PLoS One 2017 20;12(7):e0181178. Epub 2017 Jul 20.

Department of Microbiology and Molecular Genetics, University of Pittsburgh School of Medicine, Pittsburgh, Pennsylvania, United States of America.

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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0181178PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5519068PMC
October 2017

Structure-activity relationship investigation for benzonaphthyridinone derivatives as novel potent Bruton's tyrosine kinase (BTK) irreversible inhibitors.

Eur J Med Chem 2017 Sep 9;137:545-557. Epub 2017 Jun 9.

High Magnetic Field Laboratory, Chinese Academy of Sciences, Mailbox 1110, 350 Shushanhu Road, Hefei, Anhui 230031, PR China; CHMFL-HCMTC Target Therapy Joint Laboratory, 350 Shushanhu Road, Hefei Anhui 230031, PR China. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2017.06.016DOI Listing
September 2017

KRAS G12C Drug Development: Discrimination between Switch II Pocket Configurations Using Hydrogen/Deuterium-Exchange Mass Spectrometry.

Structure 2017 09 3;25(9):1442-1448.e3. Epub 2017 Aug 3.

Departments of Biochemistry and Radiation Oncology, The University of Texas Southwestern Medical Center at Dallas, Dallas, TX 75390, USA. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S09692126173021
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http://dx.doi.org/10.1016/j.str.2017.07.003DOI Listing
September 2017

Characterization of a highly selective inhibitor of the Aurora kinases.

Bioorg Med Chem Lett 2017 09 10;27(18):4405-4408. Epub 2017 Aug 10.

Department of Cancer Biology, Dana-Farber Cancer Institute, Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, USA. Electronic address:

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http://dx.doi.org/10.1016/j.bmcl.2017.08.016DOI Listing
September 2017

Discovery of a potent dual ALK and EGFR T790M inhibitor.

Eur J Med Chem 2017 Aug 3;136:497-510. Epub 2017 May 3.

Department of Biological Chemistry & Molecular Pharmacology, Harvard Medical School, Boston, MA 02115, United States; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02215, United States. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2017.04.079DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5800871PMC
August 2017

Potent and Selective Covalent Quinazoline Inhibitors of KRAS G12C.

Cell Chem Biol 2017 Aug 3;24(8):1005-1016.e3. Epub 2017 Aug 3.

Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02115, USA; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02115, USA. Electronic address:

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http://dx.doi.org/10.1016/j.chembiol.2017.06.017DOI Listing
August 2017

A UV-Independent Topical Small-Molecule Approach for Melanin Production in Human Skin.

Cell Rep 2017 06;19(11):2177-2184

Cutaneous Biology Research Center, Department of Dermatology, Massachusetts General Hospital, Harvard Medical School, Charlestown, MA 02129, USA. Electronic address:

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http://dx.doi.org/10.1016/j.celrep.2017.05.042DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5549921PMC
June 2017

A Simple Method to Identify Kinases That Regulate Embryonic Stem Cell Pluripotency by High-throughput Inhibitor Screening.

J Vis Exp 2017 05 12(123). Epub 2017 May 12.

The MRC Protein Phosphorylation and Ubiquitylation Unit, School of Life Sciences, University of Dundee;

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http://dx.doi.org/10.3791/55515DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5607952PMC
May 2017

Discoidin domain receptor 2 mediates collagen-induced activation of membrane-type 1 matrix metalloproteinase in human fibroblasts.

J Biol Chem 2017 04 7;292(16):6633-6643. Epub 2017 Mar 7.

From the Kennedy Institute of Rheumatology, Kennedy Institute of Rheumatology, University of Oxford, Roosevelt Drive, Oxford OX3 7FY, United Kingdom and

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http://dx.doi.org/10.1074/jbc.M116.770057DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5399112PMC
April 2017

Discovery of host-targeted covalent inhibitors of dengue virus.

Antiviral Res 2017 Mar 26;139:171-179. Epub 2016 Dec 26.

Department of Microbiology and Immunobiology, Harvard Medical School, Boston, MA 02115, USA. Electronic address:

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http://dx.doi.org/10.1016/j.antiviral.2016.12.017DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5373925PMC
March 2017

Structure-Activity Relationship Study of QL47: A Broad-Spectrum Antiviral Agent.

ACS Med Chem Lett 2017 Mar 3;8(3):344-349. Epub 2017 Feb 3.

Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, Massachusetts 02215, United States; Departments of Biological Chemistry & Molecular Pharmacology and Microbiology and Immunobiology, Harvard Medical School, Boston, Massachusetts 02115, United States.

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http://dx.doi.org/10.1021/acsmedchemlett.7b00008DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5346993PMC
March 2017

Identification of compounds with anti-human cytomegalovirus activity that inhibit production of IE2 proteins.

Antiviral Res 2017 02 9;138:61-67. Epub 2016 Dec 9.

Institute of Infection & Immunity, St George's, University of London, London, UK; Department of Biological Chemistry & Molecular Pharmacology, Harvard Medical School, Boston, MA, USA. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S01663542163051
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http://dx.doi.org/10.1016/j.antiviral.2016.12.006DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5244968PMC
February 2017

Structure-guided development of covalent TAK1 inhibitors.

Bioorg Med Chem 2017 02 9;25(3):838-846. Epub 2016 Dec 9.

Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02115, USA; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02215, USA. Electronic address:

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http://dx.doi.org/10.1016/j.bmc.2016.11.035DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5484537PMC
February 2017

Studies of TAK1-centered polypharmacology with novel covalent TAK1 inhibitors.

Bioorg Med Chem 2017 02 7;25(4):1320-1328. Epub 2016 Dec 7.

Department of Cancer Biology, Dana Farber Cancer Institute, Boston, MA 02115, USA; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02215, USA. Electronic address:

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http://dx.doi.org/10.1016/j.bmc.2016.11.034DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5484535PMC
February 2017

A benzo[b]thiophene-based selective type 4 S1P receptor agonist.

Bioorg Med Chem Lett 2017 01 18;27(1):1-5. Epub 2016 Nov 18.

Department of Cancer Biology, Dana-Farber Cancer Institute, Harvard Medical School, 360 Longwood Avenue, Boston, MA 02215, USA. Electronic address:

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http://dx.doi.org/10.1016/j.bmcl.2016.11.050DOI Listing
January 2017

Covalent Guanosine Mimetic Inhibitors of G12C KRAS.

ACS Med Chem Lett 2017 Jan 30;8(1):61-66. Epub 2016 Nov 30.

Department of Cancer Biology, Dana Farber Cancer Institute, 450 Brookline Avenue, Boston, Massachusetts 02115, United States; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, Massachusetts 02215, United States.

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http://pubs.acs.org/doi/10.1021/acsmedchemlett.6b00373
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http://dx.doi.org/10.1021/acsmedchemlett.6b00373DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5238463PMC
January 2017

Discovery of a Series of 5,11-Dihydro-6-benzo[]pyrimido[5,4-][1,4]diazepin-6-ones as Selective PI3K-δ/γ Inhibitors.

ACS Med Chem Lett 2016 Oct 2;7(10):908-912. Epub 2016 Aug 2.

Department of Cancer Biology, Dana-Farber Cancer Institute , Boston, Massachusetts 02215, United States.

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http://dx.doi.org/10.1021/acsmedchemlett.6b00209DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5066161PMC
October 2016