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Items: 1 to 20 of 28

1.

Click-generated triazole ureas as ultrapotent in vivo-active serine hydrolase inhibitors.

Adibekian A, Martin BR, Wang C, Hsu KL, Bachovchin DA, Niessen S, Hoover H, Cravatt BF.

Nat Chem Biol. 2011 May 15;7(7):469-78. doi: 10.1038/nchembio.579. Erratum in: Nat Chem Biol. 2012 Mar;8(3):318.

2.

Strategies for discovering and derisking covalent, irreversible enzyme inhibitors.

Johnson DS, Weerapana E, Cravatt BF.

Future Med Chem. 2010 Jun;2(6):949-64.

3.

Small-molecule inhibition of APT1 affects Ras localization and signaling.

Dekker FJ, Rocks O, Vartak N, Menninger S, Hedberg C, Balamurugan R, Wetzel S, Renner S, Gerauer M, Schölermann B, Rusch M, Kramer JW, Rauh D, Coates GW, Brunsveld L, Bastiaens PI, Waldmann H.

Nat Chem Biol. 2010 Jun;6(6):449-56. doi: 10.1038/nchembio.362. Epub 2010 Apr 25.

PMID:
20418879
4.

Bioactivation of the epidermal growth factor receptor inhibitor gefitinib: implications for pulmonary and hepatic toxicities.

Li X, Kamenecka TM, Cameron MD.

Chem Res Toxicol. 2009 Oct;22(10):1736-42. doi: 10.1021/tx900256y.

PMID:
19803472
5.

A functional screen implicates microRNA-138-dependent regulation of the depalmitoylation enzyme APT1 in dendritic spine morphogenesis.

Siegel G, Obernosterer G, Fiore R, Oehmen M, Bicker S, Christensen M, Khudayberdiev S, Leuschner PF, Busch CJ, Kane C, Hübel K, Dekker F, Hedberg C, Rengarajan B, Drepper C, Waldmann H, Kauppinen S, Greenberg ME, Draguhn A, Rehmsmeier M, Martinez J, Schratt GM.

Nat Cell Biol. 2009 Jun;11(6):705-16. doi: 10.1038/ncb1876. Epub 2009 May 24.

6.

Thioesterase activity and subcellular localization of acylprotein thioesterase 1/lysophospholipase 1.

Hirano T, Kishi M, Sugimoto H, Taguchi R, Obinata H, Ohshima N, Tatei K, Izumi T.

Biochim Biophys Acta. 2009 Aug;1791(8):797-805. doi: 10.1016/j.bbalip.2009.05.001. Epub 2009 May 9.

PMID:
19439193
7.

Identification of selective inhibitors of uncharacterized enzymes by high-throughput screening with fluorescent activity-based probes.

Bachovchin DA, Brown SJ, Rosen H, Cravatt BF.

Nat Biotechnol. 2009 Apr;27(4):387-94. doi: 10.1038/nbt.1531. Epub 2009 Mar 29. Erratum in: Nat Biotechnol. 2009 May;27(5):485.

8.

Characterization of dasatinib and its structural analogs as CYP3A4 mechanism-based inactivators and the proposed bioactivation pathways.

Li X, He Y, Ruiz CH, Koenig M, Cameron MD, Vojkovsky T.

Drug Metab Dispos. 2009 Jun;37(6):1242-50. doi: 10.1124/dmd.108.025932. Epub 2009 Mar 12. Erratum in: Drug Metab Dispos. 2009 Oct;37(10):2118. Vojkovsky, Tomas [added].

9.

Large-scale profiling of protein palmitoylation in mammalian cells.

Martin BR, Cravatt BF.

Nat Methods. 2009 Feb;6(2):135-8. doi: 10.1038/nmeth.1293. Epub 2009 Jan 11.

10.

Selectivity of inhibitors of endocannabinoid biosynthesis evaluated by activity-based protein profiling.

Hoover HS, Blankman JL, Niessen S, Cravatt BF.

Bioorg Med Chem Lett. 2008 Nov 15;18(22):5838-41. doi: 10.1016/j.bmcl.2008.06.091. Epub 2008 Jul 2.

11.

Efficient synthesis of 2-substituted-1,2,3-triazoles.

Kalisiak J, Sharpless KB, Fokin VV.

Org Lett. 2008 Aug 7;10(15):3171-4. doi: 10.1021/ol8006748. Epub 2008 Jul 3.

PMID:
18597477
12.
13.

Synthesis and evaluation of acyl protein thioesterase 1 (APT1) inhibitors.

Biel M, Deck P, Giannis A, Waldmann H.

Chemistry. 2006 May 15;12(15):4121-43.

PMID:
16528788
14.

Identification of a high-affinity binding site involved in the transport of endocannabinoids.

Moore SA, Nomikos GG, Dickason-Chesterfield AK, Schober DA, Schaus JM, Ying BP, Xu YC, Phebus L, Simmons RM, Li D, Iyengar S, Felder CC.

Proc Natl Acad Sci U S A. 2005 Dec 6;102(49):17852-7. Epub 2005 Nov 28.

15.

Development and biological evaluation of acyl protein thioesterase 1 (APT1) inhibitors.

Deck P, Pendzialek D, Biel M, Wagner M, Popkirova B, Ludolph B, Kragol G, Kuhlmann J, Giannis A, Waldmann H.

Angew Chem Int Ed Engl. 2005 Aug 5;44(31):4975-80. No abstract available.

PMID:
16003812
16.

Mechanistic basis of enzyme-targeted drugs.

Robertson JG.

Biochemistry. 2005 Apr 19;44(15):5561-71. Review. Erratum in: Biochemistry. 2005 Jun 21;44(24):8918.

PMID:
15823014
17.

Palmitoylation of intracellular signaling proteins: regulation and function.

Smotrys JE, Linder ME.

Annu Rev Biochem. 2004;73:559-87. Review.

PMID:
15189153
18.

In vitro SAR of (5-(2H)-isoxazolonyl) ureas, potent inhibitors of hormone-sensitive lipase.

Lowe DB, Magnuson S, Qi N, Campbell AM, Cook J, Hong Z, Wang M, Rodriguez M, Achebe F, Kluender H, Wong WC, Bullock WH, Salhanick AI, Witman-Jones T, Bowling ME, Keiper C, Clairmont KB.

Bioorg Med Chem Lett. 2004 Jun 21;14(12):3155-9.

PMID:
15149665
19.
20.

Discovering potent and selective reversible inhibitors of enzymes in complex proteomes.

Leung D, Hardouin C, Boger DL, Cravatt BF.

Nat Biotechnol. 2003 Jun;21(6):687-91. Epub 2003 May 12.

PMID:
12740587

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