Publications by authors named "Benjamin F Cravatt"

100Publications

ABHD4-dependent developmental anoikis safeguards the embryonic brain.

Nat Commun 2020 08 31;11(1):4363. Epub 2020 Aug 31.

Momentum Laboratory of Molecular Neurobiology, Institute of Experimental Medicine, 1450 Budapest Pf. 67., Budapest, Hungary.

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http://dx.doi.org/10.1038/s41467-020-18175-4DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7459116PMC
August 2020

Physical and Functional Analysis of the Putative Rpn13 Inhibitor RA190.

Cell Chem Biol 2020 Nov 27;27(11):1371-1382.e6. Epub 2020 Aug 27.

Department of Chemistry, The Scripps Research Institute, 130 Scripps Way, Jupiter, FL 33458, USA. Electronic address:

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http://dx.doi.org/10.1016/j.chembiol.2020.08.007DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7680414PMC
November 2020

Parallel Murine and Human Plaque Proteomics Reveals Pathways of Plaque Rupture.

Circ Res 2020 Sep 30;127(8):997-1022. Epub 2020 Jul 30.

Departments of Medicine (T.V., J.H.H., N.A., K.F., J.H., S.A.G., D.A.D.), University of Washington, Seattle.

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http://dx.doi.org/10.1161/CIRCRESAHA.120.317295DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7508285PMC
September 2020

Single-Cell Profiling and SCOPE-Seq Reveal Lineage Dynamics of Adult Ventricular-Subventricular Zone Neurogenesis and NOTUM as a Key Regulator.

Cell Rep 2020 Jun;31(12):107805

Department of Systems Biology, Columbia University Irving Medical Center, New York, NY 10032, USA; Department of Biochemistry & Molecular Biophysics, Columbia University Irving Medical Center, New York, NY 10032, USA. Electronic address:

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http://dx.doi.org/10.1016/j.celrep.2020.107805DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7396151PMC
June 2020

Inhibition of monoacylglycerol lipase reduces nicotine reward in the conditioned place preference test in male mice.

Neuropharmacology 2020 10 30;176:108170. Epub 2020 May 30.

Department of Pharmacology and Toxicology, Medical College of Virginia Campus, Virginia Commonwealth University, Richmond, VA, USA.

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http://dx.doi.org/10.1016/j.neuropharm.2020.108170DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7529882PMC
October 2020

A masked zinger to block GPX4.

Nat Chem Biol 2020 05;16(5):482-483

Department of Chemistry, The Scripps Research Institute, La Jolla, CA, USA.

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http://dx.doi.org/10.1038/s41589-020-0511-3DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7375742PMC
May 2020

Blockade of the Lysophosphatidylserine Lipase ABHD12 Potentiates Ferroptosis in Cancer Cells.

ACS Chem Biol 2020 04 20;15(4):871-877. Epub 2020 Mar 20.

Department of Chemistry, The Scripps Research Institute, La Jolla, California 92037, United States.

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http://dx.doi.org/10.1021/acschembio.0c00086DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7386317PMC
April 2020

3-Oxo-β-sultam as a Sulfonylating Chemotype for Inhibition of Serine Hydrolases and Activity-Based Protein Profiling.

ACS Chem Biol 2020 04 20;15(4):878-883. Epub 2020 Mar 20.

Department of Medicinal Chemistry, Research Institute for Medicines (iMed.ULisboa), Faculdade de Farmacia, Universidade de Lisboa, Av. Prof. Gama Pinto, 1649-003 Lisboa, Portugal.

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http://dx.doi.org/10.1021/acschembio.0c00090DOI Listing
April 2020

Cell-Based Ligand Discovery for the ENL YEATS Domain.

ACS Chem Biol 2020 04 19;15(4):895-903. Epub 2020 Mar 19.

Department of Chemistry, The Scripps Research Institute, La Jolla, California 92037, United States.

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http://dx.doi.org/10.1021/acschembio.0c00124DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7384521PMC
April 2020

Integrative X-ray Structure and Molecular Modeling for the Rationalization of Procaspase-8 Inhibitor Potency and Selectivity.

ACS Chem Biol 2020 02 23;15(2):575-586. Epub 2020 Jan 23.

Departments of Biological Chemistry and Chemistry and Biochemistry, David Geffen School of Medicine , University of California, Los Angeles , 405 Hilgard Avenue , Los Angeles , California 90095 , United States.

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http://dx.doi.org/10.1021/acschembio.0c00019DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7370820PMC
February 2020

A Chemical Proteomic Probe for the Mitochondrial Pyruvate Carrier Complex.

Angew Chem Int Ed Engl 2020 03 11;59(10):3896-3899. Epub 2020 Feb 11.

Department of Chemistry, The Scripps Research Institute, La Jolla, CA, 92037, USA.

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http://dx.doi.org/10.1002/anie.201914391DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7323913PMC
March 2020

-acyl taurines are endogenous lipid messengers that improve glucose homeostasis.

Proc Natl Acad Sci U S A 2019 12 18;116(49):24770-24778. Epub 2019 Nov 18.

Novo Nordisk Foundation Center for Basic Metabolic Research, Faculty of Health and Medical Sciences, University of Copenhagen, 2200 Copenhagen, Denmark;

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http://dx.doi.org/10.1073/pnas.1916288116DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6900532PMC
December 2019

The novel MAGL inhibitor MJN110 enhances responding to reward-predictive incentive cues by activation of CB1 receptors.

Neuropharmacology 2020 01 17;162:107814. Epub 2019 Oct 17.

Department of Pharmacology and Toxicology, Jacobs School of Medicine and Biomedical Sciences, University at Buffalo, 955 Main St, Buffalo, NY, 14203, USA. Electronic address:

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http://dx.doi.org/10.1016/j.neuropharm.2019.107814DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6983961PMC
January 2020

Oncogene Amplification in Growth Factor Signaling Pathways Renders Cancers Dependent on Membrane Lipid Remodeling.

Cell Metab 2019 09 11;30(3):525-538.e8. Epub 2019 Jul 11.

Ludwig Institute for Cancer Research, University of California, San Diego, La Jolla, CA 92093, USA; Department of Pathology, UCSD School of Medicine, La Jolla, CA 92093, USA; Moores Cancer Center, UCSD School of Medicine, La Jolla, CA 92093, USA. Electronic address:

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http://dx.doi.org/10.1016/j.cmet.2019.06.014DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6742496PMC
September 2019

The Proteome-Wide Potential for Reversible Covalency at Cysteine.

Angew Chem Int Ed Engl 2019 08 5;58(33):11385-11389. Epub 2019 Jul 5.

Department of Chemistry, The Scripps Research Institute, La Jolla, CA, 92037, USA.

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http://dx.doi.org/10.1002/anie.201905829DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6684851PMC
August 2019

Electrophilic PROTACs that degrade nuclear proteins by engaging DCAF16.

Nat Chem Biol 2019 07 17;15(7):737-746. Epub 2019 Jun 17.

The Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, La Jolla, CA, USA.

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http://dx.doi.org/10.1038/s41589-019-0279-5DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6592777PMC
July 2019

N-Acyl pyrazoles: Effective and tunable inhibitors of serine hydrolases.

Bioorg Med Chem 2019 04 11;27(8):1693-1703. Epub 2019 Mar 11.

Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 N. Torrey Pines Road, La Jolla, CA 92037, USA. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S09680896193029
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http://dx.doi.org/10.1016/j.bmc.2019.03.020DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6474344PMC
April 2019

Discovery and Optimization of Selective and in Vivo Active Inhibitors of the Lysophosphatidylserine Lipase α/β-Hydrolase Domain-Containing 12 (ABHD12).

J Med Chem 2019 02 5;62(3):1643-1656. Epub 2019 Feb 5.

Department of Chemistry , The Scripps Research Institute , 10550 N. Torrey Pines Road , La Jolla , California 92037 , United States.

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http://dx.doi.org/10.1021/acs.jmedchem.8b01958DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6583925PMC
February 2019

Global Portrait of Protein Targets of Metabolites of the Neurotoxic Compound BIA 10-2474.

ACS Chem Biol 2019 02 31;14(2):192-197. Epub 2019 Jan 31.

Department of Chemistry, The Skaggs Institute for Chemical Biology , The Scripps Research Institute , La Jolla , California 92037 , United States.

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http://pubs.acs.org/doi/10.1021/acschembio.8b01097
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http://dx.doi.org/10.1021/acschembio.8b01097DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6383364PMC
February 2019

Deficiency of Monoacylglycerol Lipase Enhances IgM Plasma Levels and Limits Atherogenesis in a CB2-Dependent Manner.

Thromb Haemost 2019 Feb 4;119(2):348-351. Epub 2019 Jan 4.

Institute for Cardiovascular Prevention (IPEK), Ludwig-Maximilians University (LMU) of Munich, Munich, Germany.

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http://dx.doi.org/10.1055/s-0038-1676769DOI Listing
February 2019

Inhibition of Protein Secretion in and Sub-MIC Effects of Arylomycin Antibiotics.

Antimicrob Agents Chemother 2019 02 29;63(2). Epub 2019 Jan 29.

Department of Chemistry, The Scripps Research Institute, La Jolla, California, USA

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http://aac.asm.org/lookup/doi/10.1128/AAC.01253-18
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http://dx.doi.org/10.1128/AAC.01253-18DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6355593PMC
February 2019

The Spastic Paraplegia-Associated Phospholipase DDHD1 Is a Primary Brain Phosphatidylinositol Lipase.

Biochemistry 2018 10 17;57(39):5759-5767. Epub 2018 Sep 17.

Department of Chemistry, The Skaggs Institute for Chemical Biology , The Scripps Research Institute , La Jolla , California 92037 , United States.

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http://dx.doi.org/10.1021/acs.biochem.8b00810DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6237197PMC
October 2018

Role of interleukin 1-beta in the inflammatory response in a fatty acid amide hydrolase-knockout mouse model of Alzheimer's disease.

Biochem Pharmacol 2018 11 6;157:202-209. Epub 2018 Sep 6.

Faculty of Experimental Sciences, Universidad Francisco de Vitoria, Pozuelo de Alarcón, 28223 Madrid, Spain. Electronic address:

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http://dx.doi.org/10.1016/j.bcp.2018.09.009DOI Listing
November 2018

Re-examining the potential of targeting ABHD6 in multiple sclerosis: Efficacy of systemic and peripherally restricted inhibitors in experimental autoimmune encephalomyelitis.

Neuropharmacology 2018 10 30;141:181-191. Epub 2018 Aug 30.

Department of Neurosciences, University of the Basque Country UPV/EHU, 48940, Leioa, Spain; Achucarro Basque Center for Neuroscience, 48940, Leioa, Spain; Centro de Investigación Biomédica en Red Sobre Enfermedades Neurodegenerativas (CIBERNED), 28029, Madrid, Spain. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S00283908183059
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http://dx.doi.org/10.1016/j.neuropharm.2018.08.038DOI Listing
October 2018

Neuroprotective effects of fatty acid amide hydrolase catabolic enzyme inhibition in a HIV-1 Tat model of neuroAIDS.

Neuropharmacology 2018 10 13;141:55-65. Epub 2018 Aug 13.

Department of Psychology & Neuroscience, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA. Electronic address:

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http://dx.doi.org/10.1016/j.neuropharm.2018.08.013DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6296377PMC
October 2018

Selective Irreversible Inhibitors of the Wnt-Deacylating Enzyme NOTUM Developed by Activity-Based Protein Profiling.

ACS Med Chem Lett 2018 Jun 26;9(6):563-568. Epub 2018 May 26.

The Skaggs Institute for Chemical Biology, Department of Chemical Physiology, The Scripps Research Institute, La Jolla, California 92037, United States.

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http://dx.doi.org/10.1021/acsmedchemlett.8b00191DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6004566PMC
June 2018

Direct Access to Versatile Electrophiles via Catalytic Oxidative Cyanation of Alkenes.

J Am Chem Soc 2018 07 22;140(26):8069-8073. Epub 2018 Jun 22.

Department of Chemistry , The Scripps Research Institute , 10550 North Torrey Pines Road , La Jolla , California 92037 , United States.

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http://dx.doi.org/10.1021/jacs.8b03704DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6033665PMC
July 2018

Discovery of Modulators of Adipocyte Physiology Using Fully Functionalized Fragments.

Methods Mol Biol 2018 ;1787:115-127

Department of Molecular Medicine, The Skaggs Institute for Chemical Biology, The Scripps Research Institute, La Jolla, CA, USA.

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http://dx.doi.org/10.1007/978-1-4939-7847-2_9DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6010189PMC
February 2019

Covalent inhibitors of nicotinamide N-methyltransferase (NNMT) provide evidence for target engagement challenges in situ.

Bioorg Med Chem Lett 2018 09 10;28(16):2682-2687. Epub 2018 Apr 10.

Department of Molecular Medicine, The Scripps Research Institute, La Jolla, CA 92307, United States. Electronic address:

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http://dx.doi.org/10.1016/j.bmcl.2018.04.017DOI Listing
September 2018

Chemistry Takes Center Stage for Identifying Cancer Targetability.

Cell 2018 05;173(4):815-817

Department of Molecular Medicine, The Scripps Research Institute, La Jolla, CA 92037, USA. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S00928674183051
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http://dx.doi.org/10.1016/j.cell.2018.04.020DOI Listing
May 2018

Proteome-wide mapping of PQS-interacting proteins in .

Chem Sci 2018 Feb 19;9(8):2290-2294. Epub 2018 Jan 19.

Dept. of Chemistry , The National Institute for Biotechnology in the Negev , Ben-Gurion University of the Negev , Be'er Sheva , Israel . Email: ; Email:

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http://dx.doi.org/10.1039/c7sc04287fDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5897874PMC
February 2018

Monoacylglycerol Lipase Inhibitors Reverse Paclitaxel-Induced Nociceptive Behavior and Proinflammatory Markers in a Mouse Model of Chemotherapy-Induced Neuropathy.

J Pharmacol Exp Ther 2018 07 14;366(1):169-183. Epub 2018 Mar 14.

Department of Pharmacology and Toxicology, Virginia Commonwealth University, Richmond, Virginia (Z.A.C., J.L.W., D.B., S.L.K., N.P., G.D., M.A.M., J.L.P., D.A.G., M.I.D., A.H.L.); The Skaggs Institute for Chemical Biology and Department of Chemical Physiology, The Scripps Research Institute, La Jolla, California (M.J.N., B.F.C.); and Department of Chemistry, University of Virginia, Charlottesville, Virginia (K.-L.H.)

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http://jpet.aspetjournals.org/lookup/doi/10.1124/jpet.117.24
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http://dx.doi.org/10.1124/jpet.117.245704DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6038031PMC
July 2018

Functional Contribution of the Spastic Paraplegia-Related Triglyceride Hydrolase DDHD2 to the Formation and Content of Lipid Droplets.

Biochemistry 2018 Feb 26;57(5):827-838. Epub 2017 Dec 26.

Department of Chemical Physiology, The Skaggs Institute for Chemical Biology, The Scripps Research Institute , La Jolla, California 92037, United States.

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http://dx.doi.org/10.1021/acs.biochem.7b01028DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5854151PMC
February 2018

"Inverse Drug Discovery" Strategy To Identify Proteins That Are Targeted by Latent Electrophiles As Exemplified by Aryl Fluorosulfates.

J Am Chem Soc 2018 01 21;140(1):200-210. Epub 2017 Dec 21.

Department of Molecular Medicine, ‡Department of Chemistry, §Department of Integrative, Structural and Computational Biology, and ∥The Skaggs Institute for Chemical Biology, The Scripps Research Institute , La Jolla, California 92037, United States.

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http://pubs.acs.org/doi/10.1021/jacs.7b08366
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http://dx.doi.org/10.1021/jacs.7b08366DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5762408PMC
January 2018

Multicomponent mapping of boron chemotypes furnishes selective enzyme inhibitors.

Nat Commun 2017 11 24;8(1):1760. Epub 2017 Nov 24.

Davenport Research Laboratories, Department of Chemistry, University of Toronto, 80 St George Street, Toronto, ON, Canada, M5S 3H6.

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http://dx.doi.org/10.1038/s41467-017-01319-4DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5701053PMC
November 2017

Global profiling of lysine reactivity and ligandability in the human proteome.

Nat Chem 2017 12 31;9(12):1181-1190. Epub 2017 Jul 31.

Department of Chemical Physiology, The Scripps Research Institute, La Jolla, California 92307, USA.

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http://dx.doi.org/10.1038/nchem.2826DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5726523PMC
December 2017

Omega-3 fatty acid epoxides are autocrine mediators that control the magnitude of IgE-mediated mast cell activation.

Nat Med 2017 Nov 9;23(11):1287-1297. Epub 2017 Oct 9.

Laboratory of Health Chemistry, Graduate School of Pharmaceutical Sciences, University of Tokyo, Tokyo, Japan.

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http://dx.doi.org/10.1038/nm.4417DOI Listing
November 2017

Investigation of Diacylglycerol Lipase Alpha Inhibition in the Mouse Lipopolysaccharide Inflammatory Pain Model.

J Pharmacol Exp Ther 2017 12 2;363(3):394-401. Epub 2017 Oct 2.

Department of Pharmacology and Toxicology, Virginia Commonwealth University, Richmond, Virginia (J.L.W., G.D., T.W.G., R.A.A., A.H.L.); and The Skaggs Institute for Chemical Biology and Department of Chemical Physiology, The Scripps Research Institute, La Jolla, California (D.O., B.F.C.).

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http://dx.doi.org/10.1124/jpet.117.243808DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5698945PMC
December 2017

Proteome-wide Map of Targets of T790M-EGFR-Directed Covalent Inhibitors.

Cell Chem Biol 2017 Nov 28;24(11):1388-1400.e7. Epub 2017 Sep 28.

Department of Molecular Medicine, The Scripps Research Institute, 10550 N. Torrey Pines Road, La Jolla, CA 92037, USA. Electronic address:

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http://dx.doi.org/10.1016/j.chembiol.2017.08.017DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5693604PMC
November 2017

Mapping Protein Targets of Bioactive Small Molecules Using Lipid-Based Chemical Proteomics.

ACS Chem Biol 2017 10 20;12(10):2671-2681. Epub 2017 Sep 20.

Department of Molecular Medicine, The Skaggs Institute for Chemical Biology, The Scripps Research Institute , La Jolla, California 92037, United States.

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http://dx.doi.org/10.1021/acschembio.7b00581DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5650530PMC
October 2017

Regulation of calcium release from the endoplasmic reticulum by the serine hydrolase ABHD2.

Biochem Biophys Res Commun 2017 09 3;490(4):1226-1231. Epub 2017 Jul 3.

Department of Pediatrics, National Jewish Health, Denver, CO, 80206, USA. Electronic address:

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http://dx.doi.org/10.1016/j.bbrc.2017.06.195DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5658124PMC
September 2017

Quantitative Chemical Proteomic Profiling of the in Vivo Targets of Reactive Drug Metabolites.

ACS Chem Biol 2017 08 21;12(8):2040-2050. Epub 2017 Jun 21.

The Skaggs Institute for Chemical Biology and Department of Chemical Physiology, The Scripps Research Institute , 10550 N. Torrey Pines Rd., La Jolla, California 92307, United States.

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http://dx.doi.org/10.1021/acschembio.7b00346DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5626524PMC
August 2017

Design of Benzoxathiazin-3-one 1,1-Dioxides as a New Class of Irreversible Serine Hydrolase Inhibitors: Discovery of a Uniquely Selective PNPLA4 Inhibitor.

J Am Chem Soc 2017 05 12;139(20):7052-7061. Epub 2017 May 12.

Departments of Chemistry, and ‡Chemical Physiology and The Skaggs Institute for Chemical Biology, The Scripps Research Institute , 10550 North Torrey Pines Road, La Jolla, California 92037, United States.

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http://dx.doi.org/10.1021/jacs.7b02985DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5501285PMC
May 2017

Chemoproteomic profiling and discovery of protein electrophiles in human cells.

Nat Chem 2017 03 31;9(3):234-243. Epub 2016 Oct 31.

Chemical Physiology, The Scripps Research Institute, La Jolla, California 92037, USA.

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http://dx.doi.org/10.1038/nchem.2645DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5325178PMC
March 2017

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

Cell 2017 01 19;168(3):517-526.e18. Epub 2017 Jan 19.

Department of Bioengineering and Therapeutic Sciences and California Institute for Quantitative Biosciences, University of California, San Francisco, San Francisco, CA 94158, USA. Electronic address:

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http://dx.doi.org/10.1016/j.cell.2016.12.021DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5302092PMC
January 2017

Ligand and Target Discovery by Fragment-Based Screening in Human Cells.

Cell 2017 01 19;168(3):527-541.e29. Epub 2017 Jan 19.

Department of Chemical Physiology, The Skaggs Institute for Chemical Biology, The Scripps Research Institute, La Jolla, CA 92037, USA. Electronic address:

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http://dx.doi.org/10.1016/j.cell.2016.12.029DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5632530PMC
January 2017

Covalent Modulators of the Vacuolar ATPase.

J Am Chem Soc 2017 01 30;139(2):639-642. Epub 2016 Dec 30.

Department of Chemical Physiology, The Scripps Research Institute , La Jolla, California 92307, United States.

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http://dx.doi.org/10.1021/jacs.6b12511DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5274637PMC
January 2017

Metabolically Labile Fumarate Esters Impart Kinetic Selectivity to Irreversible Inhibitors.

J Am Chem Soc 2016 12 5;138(49):15841-15844. Epub 2016 Dec 5.

The Skaggs Institute for Chemical Biology and Department of Chemical Physiology , 10550 North Torrey Pines Road, La Jolla, California 92037, United States.

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http://dx.doi.org/10.1021/jacs.6b10589DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5273863PMC
December 2016

Coordinated regulation of endocannabinoid-mediated retrograde synaptic suppression in the cerebellum by neuronal and astrocytic monoacylglycerol lipase.

Sci Rep 2016 10 24;6:35829. Epub 2016 Oct 24.

Department of Pharmacology and Toxicology, Medical College of Wisconsin, 8701 Watertown Plank Road, Milwaukee, WI 53226.

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http://dx.doi.org/10.1038/srep35829DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5075776PMC
October 2016

An LXR-Cholesterol Axis Creates a Metabolic Co-Dependency for Brain Cancers.

Cancer Cell 2016 Nov 13;30(5):683-693. Epub 2016 Oct 13.

Ludwig Institute for Cancer Research, University of California San Diego, La Jolla, CA 92093, USA; Department of Pathology, UCSD School of Medicine, La Jolla, CA 92093, USA; Moores Cancer Center, UCSD School of Medicine, La Jolla, CA 92093, USA. Electronic address:

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http://dx.doi.org/10.1016/j.ccell.2016.09.008DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5479636PMC
November 2016

Chemical Proteomic Profiling of Human Methyltransferases.

J Am Chem Soc 2016 10 30;138(40):13335-13343. Epub 2016 Sep 30.

Departments of Chemical Physiology, The Scripps Research Institute , La Jolla, California 92307, United States.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5072128PMC
http://dx.doi.org/10.1021/jacs.6b07830DOI Listing
October 2016

Chemical proteomic map of dimethyl fumarate-sensitive cysteines in primary human T cells.

Sci Signal 2016 09 13;9(445):rs10. Epub 2016 Sep 13.

Department of Chemical Physiology and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5068918PMC
http://dx.doi.org/10.1126/scisignal.aaf7694DOI Listing
September 2016

Discovery of Enzymatic Targets of Transcriptional Activators via in Vivo Covalent Chemical Capture.

J Am Chem Soc 2016 09 20;138(38):12629-35. Epub 2016 Sep 20.

The Skaggs Institute for Chemical Biology and Department of Chemical Physiology, The Scripps Research Institute , La Jolla, California 92037, United States.

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http://dx.doi.org/10.1021/jacs.6b07680DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5217703PMC
September 2016

Branched Fatty Acid Esters of Hydroxy Fatty Acids Are Preferred Substrates of the MODY8 Protein Carboxyl Ester Lipase.

Biochemistry 2016 08 10;55(33):4636-41. Epub 2016 Aug 10.

Peptide Biology Laboratories, Helmsley Center for Genomic Medicine, Salk Institute for Biological Studies , La Jolla, California 92037, United States.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5056623PMC
http://dx.doi.org/10.1021/acs.biochem.6b00565DOI Listing
August 2016

Robust anti-nociceptive effects of monoacylglycerol lipase inhibition in a model of osteoarthritis pain.

Br J Pharmacol 2016 11 23;173(21):3134-3144. Epub 2016 Sep 23.

Arthritis Research UK Pain Centre, University of Nottingham, Medical School, Queen's Medical Centre, Nottingham, UK.

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http://dx.doi.org/10.1111/bph.13574DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5056226PMC
November 2016

Synthesis and Sulfur Electrophilicity of the Nuphar Thiaspirane Pharmacophore.

ACS Cent Sci 2016 Jun 13;2(6):401-8. Epub 2016 Jun 13.

Department of Chemistry, The Scripps Research Institute , 10550 North Torrey Pines Road, La Jolla, California 92037, United States.

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http://dx.doi.org/10.1021/acscentsci.6b00113DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4919772PMC
June 2016

A calcium-dependent acyltransferase that produces N-acyl phosphatidylethanolamines.

Nat Chem Biol 2016 09 11;12(9):669-71. Epub 2016 Jul 11.

Department of Chemical Physiology, The Scripps Research Institute, La Jolla, California, USA.

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http://dx.doi.org/10.1038/nchembio.2127DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4990470PMC
September 2016

Just add water: cannabinoid discrimination in a water T-maze with FAAH(-/-) and FAAH(+/+) mice.

Behav Pharmacol 2016 08;27(5):479-84

aRTI International, Research Triangle Park, North CarolinabThe Skaggs Institute for Chemical Biology and Department of Chemical Physiology, The Scripps Research Institute, La Jolla, CaliforniacDepartment of Pharmacology and Toxicology, Virginia Commonwealth University, Richmond, Virginia, USA.

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http://dx.doi.org/10.1097/FBP.0000000000000228DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4937884PMC
August 2016

Paracrine Induction of HIF by Glutamate in Breast Cancer: EglN1 Senses Cysteine.

Cell 2016 Jun;166(1):126-39

Department of Medical Oncology, Dana-Farber Cancer Institute and Brigham and Women's Hospital, Boston, MA 02215, USA; Howard Hughes Medical Institute, Chevy Chase, MD 20815, USA. Electronic address:

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http://dx.doi.org/10.1016/j.cell.2016.05.042DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4930557PMC
June 2016

Discriminative Stimulus Properties of the Endocannabinoid Catabolic Enzyme Inhibitor SA-57 in Mice.

J Pharmacol Exp Ther 2016 08 15;358(2):306-14. Epub 2016 Jun 15.

Department of Pharmacology and Toxicology, Medical College of Virginia Campus, Virginia Commonwealth University, Richmond, Virginia (R.A.O., B.I.J., M.M., P.M.B., A.J., D.E.S., A.H.L.); RTI International, Research Triangle Park, North Carolina (J.L.W.); and The Skaggs Institute for Chemical Biology and Department of Chemical Physiology, The Scripps Research Institute, La Jolla, California (M.J.N.; B.F.C.)

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http://jpet.aspetjournals.org/content/early/2016/06/15/jpet.
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http://link.springer.com/content/pdf/10.1007%2F7854_2016_24.
Web Search
http://jpet.aspetjournals.org/cgi/doi/10.1124/jpet.115.22949
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http://dx.doi.org/10.1124/jpet.115.229492DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4959103PMC
August 2016

Arylfluorosulfates Inactivate Intracellular Lipid Binding Protein(s) through Chemoselective SuFEx Reaction with a Binding Site Tyr Residue.

J Am Chem Soc 2016 06 2;138(23):7353-64. Epub 2016 Jun 2.

Department of Chemistry and §Department of Molecular and Experimental Medicine, ∥Department of Chemical Physiology, ⊥Department of Integrative Structural and Computational Biology, #The Skaggs Institute for Chemical Biology, The Scripps Research Institute , La Jolla, California 92037, United States.

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http://dx.doi.org/10.1021/jacs.6b02960DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4909538PMC
June 2016