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Items: 1 to 50 of 481

1.

Dimethyl Fumarate Disrupts Human Innate Immune Signaling by Targeting the IRAK4-MyD88 Complex.

Zaro BW, Vinogradova EV, Lazar DC, Blewett MM, Suciu RM, Takaya J, Studer S, de la Torre JC, Casanova JL, Cravatt BF, Teijaro JR.

J Immunol. 2019 Mar 18. pii: ji1801627. doi: 10.4049/jimmunol.1801627. [Epub ahead of print]

PMID:
30885957
2.

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

Otrubova K, Chatterjee S, Ghimire S, Cravatt BF, Boger DL.

Bioorg Med Chem. 2019 Mar 11. pii: S0968-0896(19)30292-5. doi: 10.1016/j.bmc.2019.03.020. [Epub ahead of print]

PMID:
30879861
3.

Design, Synthesis, and Evaluation of Reversible and Irreversible Monoacylglycerol Lipase Positron Emission Tomography (PET) Tracers Using a "Tail Switching" Strategy on a Piperazinyl Azetidine Skeleton.

Chen Z, Mori W, Deng X, Cheng R, Ogasawara D, Zhang G, Schafroth MA, Dahl K, Fu H, Hatori A, Shao T, Zhang Y, Yamasaki T, Zhang X, Rong J, Yu Q, Hu K, Fujinaga M, Xie L, Kumata K, Gou Y, Chen J, Gu S, Bao L, Wang L, Collier TL, Vasdev N, Shao Y, Ma JA, Cravatt BF, Fowler C, Josephson L, Zhang MR, Liang SH.

J Med Chem. 2019 Mar 21. doi: 10.1021/acs.jmedchem.8b01778. [Epub ahead of print]

PMID:
30829483
4.

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

Ogasawara D, Ichu TA, Jing H, Hulce JJ, Reed A, Ulanovskaya OA, Cravatt BF.

J Med Chem. 2019 Feb 5. doi: 10.1021/acs.jmedchem.8b01958. [Epub ahead of print]

PMID:
30720278
5.

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

Huang Z, Ogasawara D, Seneviratne UI, Cognetta AB 3rd, Am Ende CW, Nason DM, Lapham K, Litchfield J, Johnson DS, Cravatt BF.

ACS Chem Biol. 2019 Feb 15;14(2):192-197. doi: 10.1021/acschembio.8b01097. Epub 2019 Jan 31.

PMID:
30702848
6.

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

Guillamat Prats R, Rami M, Ring L, Rinne P, Lauer E, Lenglet S, Thomas A, Pagano S, Vuilleumier N, Cravatt BF, Weber C, Faussner A, Steffens S.

Thromb Haemost. 2019 Feb;119(2):348-351. doi: 10.1055/s-0038-1676769. Epub 2019 Jan 4.

PMID:
30609444
7.

Translation attenuation by minocycline enhances longevity and proteostasis in old post-stress-responsive organisms.

Solis GM, Kardakaris R, Valentine ER, Bar-Peled L, Chen AL, Blewett MM, McCormick MA, Williamson JR, Kennedy B, Cravatt BF, Petrascheck M.

Elife. 2018 Nov 27;7. pii: e40314. doi: 10.7554/eLife.40314.

8.

Ethanol-induced alterations in endocannabinoids and relevant neurotransmitters in the nucleus accumbens of fatty acid amide hydrolase knockout mice.

Pavón FJ, Serrano A, Stouffer DG, Polis I, Roberto M, Cravatt BF, Martin-Fardon R, Rodríguez de Fonseca F, Parsons LH.

Addict Biol. 2018 Nov 13. doi: 10.1111/adb.12695. [Epub ahead of print]

PMID:
30421483
9.

Selective blockade of the lyso-PS lipase ABHD12 stimulates immune responses in vivo.

Ogasawara D, Ichu TA, Vartabedian VF, Benthuysen J, Jing H, Reed A, Ulanovskaya OA, Hulce JJ, Roberts A, Brown S, Rosen H, Teijaro JR, Cravatt BF.

Nat Chem Biol. 2018 Dec;14(12):1099-1108. doi: 10.1038/s41589-018-0155-8. Epub 2018 Nov 12.

PMID:
30420694
10.

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

Walsh SI, Peters DS, Smith PA, Craney A, Dix MM, Cravatt BF, Romesberg FE.

Antimicrob Agents Chemother. 2019 Jan 29;63(2). pii: e01253-18. doi: 10.1128/AAC.01253-18. Print 2019 Feb.

PMID:
30420476
11.

Inhibition of monoacylglycerol lipase, an anti-inflammatory and antifibrogenic strategy in the liver.

Habib A, Chokr D, Wan J, Hegde P, Mabire M, Siebert M, Ribeiro-Parenti L, Le Gall M, Lettéron P, Pilard N, Mansouri A, Brouillet A, Tardelli M, Weiss E, Le Faouder P, Guillou H, Cravatt BF, Moreau R, Trauner M, Lotersztajn S.

Gut. 2018 Oct 9. pii: gutjnl-2018-316137. doi: 10.1136/gutjnl-2018-316137. [Epub ahead of print]

PMID:
30301768
12.

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

Inloes JM, Jing H, Cravatt BF.

Biochemistry. 2018 Oct 2;57(39):5759-5767. doi: 10.1021/acs.biochem.8b00810. Epub 2018 Sep 17.

PMID:
30221923
13.

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

Aparicio N, Grande MT, Ruiz de Martín Esteban S, López A, Ruiz-Pérez G, Amores M, Vázquez C, Martínez-Relimpio AM, Pazos MR, Cravatt BF, Tolón RM, Romero J.

Biochem Pharmacol. 2018 Nov;157:202-209. doi: 10.1016/j.bcp.2018.09.009. Epub 2018 Sep 6.

PMID:
30195729
14.

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

Manterola A, Bernal-Chico A, Cipriani R, Ruiz A, Pérez-Samartín A, Moreno-Rodríguez M, Hsu KL, Cravatt BF, Brown JM, Rodríguez-Puertas R, Matute C, Mato S.

Neuropharmacology. 2018 Oct;141:181-191. doi: 10.1016/j.neuropharm.2018.08.038. Epub 2018 Aug 30.

PMID:
30171986
15.

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

Hermes DJ, Xu C, Poklis JL, Niphakis MJ, Cravatt BF, Mackie K, Lichtman AH, Ignatowska-Jankowska BM, Fitting S.

Neuropharmacology. 2018 Oct;141:55-65. doi: 10.1016/j.neuropharm.2018.08.013. Epub 2018 Aug 13.

16.

Endocannabinoid regulation of homeostatic feeding and stress-induced alterations in food intake in male rats.

Sticht MA, Lau DJ, Keenan CM, Cavin JB, Morena M, Vemuri VK, Makriyannis A, Cravatt BF, Sharkey KA, Hill MN.

Br J Pharmacol. 2018 Jul 26. doi: 10.1111/bph.14453. [Epub ahead of print]

PMID:
30051485
17.

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.

18.

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
19.

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 Aug;43(9):1840-1850. doi: 10.1038/s41386-018-0055-3. Epub 2018 Apr 5.

PMID:
29748627
20.

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.

21.

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 Sep 1;28(16):2682-2687. doi: 10.1016/j.bmcl.2018.04.017. Epub 2018 Apr 10.

PMID:
29731364
22.

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
23.

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.

24.

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
25.

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
26.

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.

27.

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.

28.

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.

29.

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.

30.

"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.

31.

Multicomponent mapping of boron chemotypes furnishes selective enzyme inhibitors.

Tan J, Cognetta Iii AB, 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.

32.

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.

33.

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. 2018 Jul 15;84(2):85-94. doi: 10.1016/j.biopsych.2017.09.024. Epub 2017 Oct 6.

PMID:
29100630
34.

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
35.

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.

36.

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.

37.

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.

38.

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.

39.

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.

40.

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.

41.

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.

42.

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.

43.

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.

44.

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.

45.

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.

46.

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.

47.

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.

48.

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.

49.

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.

50.

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.

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