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Items: 1 to 50 of 465

1.

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

Suciu RM, Cognetta AB 3rd, Potter ZE, Cravatt BF.

ACS Med Chem Lett. 2018 May 26;9(6):563-568. doi: 10.1021/acsmedchemlett.8b00191. eCollection 2018 Jun 14.

2.

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

Gao DW, Vinogradova EV, Nimmagadda SK, Medina JM, Xiao Y, Suciu RM, Cravatt BF, Engle KM.

J Am Chem Soc. 2018 Jul 5;140(26):8069-8073. doi: 10.1021/jacs.8b03704. Epub 2018 Jun 22.

PMID:
29894184
3.

Deficient endocannabinoid signaling in the central amygdala contributes to alcohol dependence-related anxiety-like behavior and excessive alcohol intake.

Serrano A, Pavon FJ, Buczynski MW, Schlosburg J, Natividad LA, Polis IY, Stouffer DG, Zorrilla EP, Roberto M, Cravatt BF, Martin-Fardon R, Rodriguez de Fonseca F, Parsons LH.

Neuropsychopharmacology. 2018 Apr 5. doi: 10.1038/s41386-018-0055-3. [Epub ahead of print]

PMID:
29748627
4.

Discovery of Modulators of Adipocyte Physiology Using Fully Functionalized Fragments.

Galmozzi A, Parker CG, Kok BP, Cravatt BF, Saez E.

Methods Mol Biol. 2018;1787:115-127. doi: 10.1007/978-1-4939-7847-2_9.

PMID:
29736714
5.

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

Lee HY, Suciu RM, Horning BD, Vinogradova EV, Ulanovskaya OA, Cravatt BF.

Bioorg Med Chem Lett. 2018 Apr 10. pii: S0960-894X(18)30324-X. doi: 10.1016/j.bmcl.2018.04.017. [Epub ahead of print]

PMID:
29731364
6.

Chemistry Takes Center Stage for Identifying Cancer Targetability.

Parker CG, Cravatt BF.

Cell. 2018 May 3;173(4):815-817. doi: 10.1016/j.cell.2018.04.020.

PMID:
29727668
7.

Proteome-wide mapping of PQS-interacting proteins in Pseudomonas aeruginosa.

Dandela R, Mantin D, Cravatt BF, Rayo J, Meijler MM.

Chem Sci. 2018 Jan 19;9(8):2290-2294. doi: 10.1039/c7sc04287f. eCollection 2018 Feb 28.

8.

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

Curry ZA, Wilkerson JL, Bagdas D, Kyte SL, Patel N, Donvito G, Mustafa MA, Poklis JL, Niphakis MJ, Hsu KL, Cravatt BF, Gewirtz DA, Damaj MI, Lichtman AH.

J Pharmacol Exp Ther. 2018 Jul;366(1):169-183. doi: 10.1124/jpet.117.245704. Epub 2018 Mar 14.

PMID:
29540562
9.

Evaluation of different drug classes on transient sciatic nerve injury-depressed marble burying in mice.

Wilkerson JL, Curry ZA, Kinlow PD, Mason BL, Hsu KL, van der Stelt M, Cravatt BF, Lichtman AH.

Pain. 2018 Jun;159(6):1155-1165. doi: 10.1097/j.pain.0000000000001199.

PMID:
29528965
10.

In Vitro and in Vivo Evaluation of 11C-Labeled Azetidinecarboxylates for Imaging Monoacylglycerol Lipase by PET Imaging Studies.

Cheng R, Mori W, Ma L, Alhouayek M, Hatori A, Zhang Y, Ogasawara D, Yuan G, Chen Z, Zhang X, Shi H, Yamasaki T, Xie L, Kumata K, Fujinaga M, Nagai Y, Minamimoto T, Svensson M, Wang L, Du Y, Ondrechen MJ, Vasdev N, Cravatt BF, Fowler C, Zhang MR, Liang SH.

J Med Chem. 2018 Mar 22;61(6):2278-2291. doi: 10.1021/acs.jmedchem.7b01400. Epub 2018 Mar 9.

PMID:
29481079
11.

How many human proteoforms are there?

Aebersold R, Agar JN, Amster IJ, Baker MS, Bertozzi CR, Boja ES, Costello CE, Cravatt BF, Fenselau C, Garcia BA, Ge Y, Gunawardena J, Hendrickson RC, Hergenrother PJ, Huber CG, Ivanov AR, Jensen ON, Jewett MC, Kelleher NL, Kiessling LL, Krogan NJ, Larsen MR, Loo JA, Ogorzalek Loo RR, Lundberg E, MacCoss MJ, Mallick P, Mootha VK, Mrksich M, Muir TW, Patrie SM, Pesavento JJ, Pitteri SJ, Rodriguez H, Saghatelian A, Sandoval W, Schlüter H, Sechi S, Slavoff SA, Smith LM, Snyder MP, Thomas PM, Uhlén M, Van Eyk JE, Vidal M, Walt DR, White FM, Williams ER, Wohlschlager T, Wysocki VH, Yates NA, Young NL, Zhang B.

Nat Chem Biol. 2018 Feb 14;14(3):206-214. doi: 10.1038/nchembio.2576.

PMID:
29443976
12.

Chemical Proteomics Identifies SLC25A20 as a Functional Target of the Ingenol Class of Actinic Keratosis Drugs.

Parker CG, Kuttruff CA, Galmozzi A, Jørgensen L, Yeh CH, Hermanson DJ, Wang Y, Artola M, McKerrall SJ, Josyln CM, Nørremark B, Dünstl G, Felding J, Saez E, Baran PS, Cravatt BF.

ACS Cent Sci. 2017 Dec 27;3(12):1276-1285. doi: 10.1021/acscentsci.7b00420. Epub 2017 Dec 6.

13.

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

Inloes JM, Kiosses WB, Wang H, Walther TC, Farese RV Jr, Cravatt BF.

Biochemistry. 2018 Feb 6;57(5):827-838. doi: 10.1021/acs.biochem.7b01028. Epub 2017 Dec 26.

PMID:
29278326
14.

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

Mortenson DE, Brighty GJ, Plate L, Bare G, Chen W, Li S, Wang H, Cravatt BF, Forli S, Powers ET, Sharpless KB, Wilson IA, Kelly JW.

J Am Chem Soc. 2018 Jan 10;140(1):200-210. doi: 10.1021/jacs.7b08366. Epub 2017 Dec 21.

PMID:
29265822
15.

Multicomponent mapping of boron chemotypes furnishes selective enzyme inhibitors.

Tan J, Cognetta AB III, Diaz DB, Lum KM, Adachi S, Kundu S, Cravatt BF, Yudin AK.

Nat Commun. 2017 Nov 24;8(1):1760. doi: 10.1038/s41467-017-01319-4.

16.

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

Hacker SM, Backus KM, Lazear MR, Forli S, Correia BE, Cravatt BF.

Nat Chem. 2017 Dec;9(12):1181-1190. doi: 10.1038/nchem.2826. Epub 2017 Jul 31.

17.

Stress Promotes Drug Seeking Through Glucocorticoid-Dependent Endocannabinoid Mobilization in the Prelimbic Cortex.

McReynolds JR, Doncheck EM, Li Y, Vranjkovic O, Graf EN, Ogasawara D, Cravatt BF, Baker DA, Liu QS, Hillard CJ, Mantsch JR.

Biol Psychiatry. 2017 Oct 6. pii: S0006-3223(17)32046-2. doi: 10.1016/j.biopsych.2017.09.024. [Epub ahead of print]

PMID:
29100630
18.

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

Shimanaka Y, Kono N, Taketomi Y, Arita M, Okayama Y, Tanaka Y, Nishito Y, Mochizuki T, Kusuhara H, Adibekian A, Cravatt BF, Murakami M, Arai H.

Nat Med. 2017 Nov;23(11):1287-1297. doi: 10.1038/nm.4417. Epub 2017 Oct 9.

PMID:
29035365
19.

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

Wilkerson JL, Donvito G, Grim TW, Abdullah RA, Ogasawara D, Cravatt BF, Lichtman AH.

J Pharmacol Exp Ther. 2017 Dec;363(3):394-401. doi: 10.1124/jpet.117.243808. Epub 2017 Oct 2.

PMID:
28970359
20.

Chemical Proteomics Identifies Druggable Vulnerabilities in a Genetically Defined Cancer.

Bar-Peled L, Kemper EK, Suciu RM, Vinogradova EV, Backus KM, Horning BD, Paul TA, Ichu TA, Svensson RU, Olucha J, Chang MW, Kok BP, Zhu Z, Ihle NT, Dix MM, Jiang P, Hayward MM, Saez E, Shaw RJ, Cravatt BF.

Cell. 2017 Oct 19;171(3):696-709.e23. doi: 10.1016/j.cell.2017.08.051. Epub 2017 Sep 28.

21.

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

Niessen S, Dix MM, Barbas S, Potter ZE, Lu S, Brodsky O, Planken S, Behenna D, Almaden C, Gajiwala KS, Ryan K, Ferre R, Lazear MR, Hayward MM, Kath JC, Cravatt BF.

Cell Chem Biol. 2017 Nov 16;24(11):1388-1400.e7. doi: 10.1016/j.chembiol.2017.08.017. Epub 2017 Sep 28.

PMID:
28965727
22.

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

Lum KM, Sato Y, Beyer BA, Plaisted WC, Anglin JL, Lairson LL, Cravatt BF.

ACS Chem Biol. 2017 Oct 20;12(10):2671-2681. doi: 10.1021/acschembio.7b00581. Epub 2017 Sep 20.

PMID:
28930429
23.

Peptide probes detect misfolded transthyretin oligomers in plasma of hereditary amyloidosis patients.

Schonhoft JD, Monteiro C, Plate L, Eisele YS, Kelly JM, Boland D, Parker CG, Cravatt BF, Teruya S, Helmke S, Maurer M, Berk J, Sekijima Y, Novais M, Coelho T, Powers ET, Kelly JW.

Sci Transl Med. 2017 Sep 13;9(407). pii: eaam7621. doi: 10.1126/scitranslmed.aam7621.

PMID:
28904227
24.

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

Yun B, Lee H, Powell R, Reisdorph N, Ewing H, Gelb MH, Hsu KL, Cravatt BF, Leslie CC.

Biochem Biophys Res Commun. 2017 Sep 2;490(4):1226-1231. doi: 10.1016/j.bbrc.2017.06.195. Epub 2017 Jul 3.

PMID:
28684316
25.

Inhibition of the endocannabinoid-regulating enzyme monoacylglycerol lipase elicits a CB1 receptor-mediated discriminative stimulus in mice.

Owens RA, Mustafa MA, Ignatowska-Jankowska BM, Damaj MI, Beardsley PM, Wiley JL, Niphakis MJ, Cravatt BF, Lichtman AH.

Neuropharmacology. 2017 Oct;125:80-86. doi: 10.1016/j.neuropharm.2017.06.032. Epub 2017 Jun 30.

PMID:
28673548
26.

Fatty acid amide hydrolase (FAAH) inactivation confers enhanced sensitivity to nicotine-induced dopamine release in the mouse nucleus accumbens.

Pavon FJ, Serrano A, Sidhpura N, Polis I, Stouffer D, de Fonseca FR, Cravatt BF, Martin-Fardon R, Parsons LH.

Addict Biol. 2018 Mar;23(2):723-734. doi: 10.1111/adb.12531. Epub 2017 Jun 29.

PMID:
28660730
27.

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

Whitby LR, Obach RS, Simon GM, Hayward MM, Cravatt BF.

ACS Chem Biol. 2017 Aug 18;12(8):2040-2050. doi: 10.1021/acschembio.7b00346. Epub 2017 Jun 21.

PMID:
28636309
28.

Activity-based protein profiling reveals off-target proteins of the FAAH inhibitor BIA 10-2474.

van Esbroeck ACM, Janssen APA, Cognetta AB 3rd, Ogasawara D, Shpak G, van der Kroeg M, Kantae V, Baggelaar MP, de Vrij FMS, Deng H, Allarà M, Fezza F, Lin Z, van der Wel T, Soethoudt M, Mock ED, den Dulk H, Baak IL, Florea BI, Hendriks G, De Petrocellis L, Overkleeft HS, Hankemeier T, De Zeeuw CI, Di Marzo V, Maccarrone M, Cravatt BF, Kushner SA, van der Stelt M.

Science. 2017 Jun 9;356(6342):1084-1087. doi: 10.1126/science.aaf7497.

29.

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

Kornahrens AF, Cognetta AB 3rd, Brody DM, Matthews ML, Cravatt BF, Boger DL.

J Am Chem Soc. 2017 May 24;139(20):7052-7061. doi: 10.1021/jacs.7b02985. Epub 2017 May 12.

30.

A Screen for Protein-Protein Interactions in Live Mycobacteria Reveals a Functional Link between the Virulence-Associated Lipid Transporter LprG and the Mycolyltransferase Antigen 85A.

Touchette MH, Van Vlack ER, Bai L, Kim J, Cognetta AB 3rd, Previti ML, Backus KM, Martin DW, Cravatt BF, Seeliger JC.

ACS Infect Dis. 2017 May 12;3(5):336-348. doi: 10.1021/acsinfecdis.6b00179. Epub 2017 Mar 21.

31.

Chemoproteomic profiling and discovery of protein electrophiles in human cells.

Matthews ML, He L, Horning BD, Olson EJ, Correia BE, Yates JR 3rd, Dawson PE, Cravatt BF.

Nat Chem. 2017 Mar;9(3):234-243. doi: 10.1038/nchem.2645. Epub 2016 Oct 31.

32.

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

Guo CJ, Chang FY, Wyche TP, Backus KM, Acker TM, Funabashi M, Taketani M, Donia MS, Nayfach S, Pollard KS, Craik CS, Cravatt BF, Clardy J, Voigt CA, Fischbach MA.

Cell. 2017 Jan 26;168(3):517-526.e18. doi: 10.1016/j.cell.2016.12.021. Epub 2017 Jan 19.

33.

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

Parker CG, Galmozzi A, Wang Y, Correia BE, Sasaki K, Joslyn CM, Kim AS, Cavallaro CL, Lawrence RM, Johnson SR, Narvaiza I, Saez E, Cravatt BF.

Cell. 2017 Jan 26;168(3):527-541.e29. doi: 10.1016/j.cell.2016.12.029. Epub 2017 Jan 19.

34.

Covalent Modulators of the Vacuolar ATPase.

Chen YC, Backus KM, Merkulova M, Yang C, Brown D, Cravatt BF, Zhang C.

J Am Chem Soc. 2017 Jan 18;139(2):639-642. doi: 10.1021/jacs.6b12511. Epub 2016 Dec 30.

35.

Triazole Ureas Act as Diacylglycerol Lipase Inhibitors and Prevent Fasting-Induced Refeeding.

Deng H, Kooijman S, van den Nieuwendijk AM, Ogasawara D, van der Wel T, van Dalen F, Baggelaar MP, Janssen FJ, van den Berg RJ, den Dulk H, Cravatt BF, Overkleeft HS, Rensen PC, van der Stelt M.

J Med Chem. 2017 Jan 12;60(1):428-440. doi: 10.1021/acs.jmedchem.6b01482. Epub 2016 Dec 19.

PMID:
27992221
36.

Metabolically Labile Fumarate Esters Impart Kinetic Selectivity to Irreversible Inhibitors.

Zaro BW, Whitby LR, Lum KM, Cravatt BF.

J Am Chem Soc. 2016 Dec 14;138(49):15841-15844. Epub 2016 Dec 5.

37.

The endocannabinoid hydrolysis inhibitor SA-57: Intrinsic antinociceptive effects, augmented morphine-induced antinociception, and attenuated heroin seeking behavior in mice.

Wilkerson JL, Ghosh S, Mustafa M, Abdullah RA, Niphakis MJ, Cabrera R, Maldonado RL, Cravatt BF, Lichtman AH.

Neuropharmacology. 2017 Mar 1;114:156-167. doi: 10.1016/j.neuropharm.2016.11.015. Epub 2016 Nov 25.

38.

Mice lacking lipid droplet-associated hydrolase, a gene linked to human prostate cancer, have normal cholesterol ester metabolism.

Kory N, Grond S, Kamat SS, Li Z, Krahmer N, Chitraju C, Zhou P, Fröhlich F, Semova I, Ejsing C, Zechner R, Cravatt BF, Farese RV Jr, Walther TC.

J Lipid Res. 2017 Jan;58(1):226-235. doi: 10.1194/jlr.M072538. Epub 2016 Nov 11.

39.

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

Liu X, Chen Y, Vickstrom CR, Li Y, Viader A, Cravatt BF, Liu QS.

Sci Rep. 2016 Oct 24;6:35829. doi: 10.1038/srep35829.

40.

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

Villa GR, Hulce JJ, Zanca C, Bi J, Ikegami S, Cahill GL, Gu Y, Lum KM, Masui K, Yang H, Rong X, Hong C, Turner KM, Liu F, Hon GC, Jenkins D, Martini M, Armando AM, Quehenberger O, Cloughesy TF, Furnari FB, Cavenee WK, Tontonoz P, Gahman TC, Shiau AK, Cravatt BF, Mischel PS.

Cancer Cell. 2016 Nov 14;30(5):683-693. doi: 10.1016/j.ccell.2016.09.008. Epub 2016 Oct 13.

41.

Chemical Proteomic Profiling of Human Methyltransferases.

Horning BD, Suciu RM, Ghadiri DA, Ulanovskaya OA, Matthews ML, Lum KM, Backus KM, Brown SJ, Rosen H, Cravatt BF.

J Am Chem Soc. 2016 Oct 12;138(40):13335-13343. Epub 2016 Sep 30.

42.

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

Blewett MM, Xie J, Zaro BW, Backus KM, Altman A, Teijaro JR, Cravatt BF.

Sci Signal. 2016 Sep 13;9(445):rs10. doi: 10.1126/scisignal.aaf7694.

43.

An in vivo multiplexed small-molecule screening platform.

Grüner BM, Schulze CJ, Yang D, Ogasawara D, Dix MM, Rogers ZN, Chuang CH, McFarland CD, Chiou SH, Brown JM, Cravatt BF, Bogyo M, Winslow MM.

Nat Methods. 2016 Oct;13(10):883-889. doi: 10.1038/nmeth.3992. Epub 2016 Sep 12.

44.

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

Dugan A, Majmudar CY, Pricer R, Niessen S, Lancia JK, Fung HY, Cravatt BF, Mapp AK.

J Am Chem Soc. 2016 Sep 28;138(38):12629-35. doi: 10.1021/jacs.6b07680. Epub 2016 Sep 20.

45.

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

Kolar MJ, Kamat SS, Parsons WH, Homan EA, Maher T, Peroni OD, Syed I, Fjeld K, Molven A, Kahn BB, Cravatt BF, Saghatelian A.

Biochemistry. 2016 Aug 23;55(33):4636-41. doi: 10.1021/acs.biochem.6b00565. Epub 2016 Aug 10.

46.

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

Burston JJ, Mapp PI, Sarmad S, Barrett DA, Niphakis MJ, Cravatt BF, Walsh DA, Chapman V.

Br J Pharmacol. 2016 Nov;173(21):3134-3144. doi: 10.1111/bph.13574. Epub 2016 Sep 23.

47.

Synthesis and Sulfur Electrophilicity of the Nuphar Thiaspirane Pharmacophore.

Tada N, Jansen DJ, Mower MP, Blewett MM, Umotoy JC, Cravatt BF, Wolan DW, Shenvi RA.

ACS Cent Sci. 2016 Jun 22;2(6):401-8. doi: 10.1021/acscentsci.6b00113. Epub 2016 Jun 13.

48.

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

Ogura Y, Parsons WH, Kamat SS, Cravatt BF.

Nat Chem Biol. 2016 Sep;12(9):669-71. doi: 10.1038/nchembio.2127. Epub 2016 Jul 11.

49.

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

Wiley JL, Lefever TW, Pulley NS, Marusich JA, Cravatt BF, Lichtman AH.

Behav Pharmacol. 2016 Aug;27(5):479-84. doi: 10.1097/FBP.0000000000000228.

50.

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

Briggs KJ, Koivunen P, Cao S, Backus KM, Olenchock BA, Patel H, Zhang Q, Signoretti S, Gerfen GJ, Richardson AL, Witkiewicz AK, Cravatt BF, Clardy J, Kaelin WG Jr.

Cell. 2016 Jun 30;166(1):126-39. doi: 10.1016/j.cell.2016.05.042.

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