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Items: 23

1.

Monoacylglycerol Lipase Inhibition in Human and Rodent Systems Supports Clinical Evaluation of Endocannabinoid Modulators.

Clapper JR, Henry CL, Niphakis MJ, Knize AM, Coppola AR, Simon GM, Ngo N, Herbst RA, Herbst DM, Reed AW, Cisar JS, Weber OD, Viader A, Alexander JP, Cunningham ML, Jones TK, Fraser IP, Grice CA, Ezekowitz RAB, O'Neill GP, Blankman JL.

J Pharmacol Exp Ther. 2018 Oct 10. pii: jpet.118.252296. doi: 10.1124/jpet.118.252296. [Epub ahead of print]

2.

Identification of ABX-1431, a Selective Inhibitor of Monoacylglycerol Lipase and Clinical Candidate for Treatment of Neurological Disorders.

Cisar JS, Weber OD, Clapper JR, Blankman JL, Henry CL, Simon GM, Alexander JP, Jones TK, Ezekowitz RAB, O'Neill GP, Grice CA.

J Med Chem. 2018 Oct 25;61(20):9062-9084. doi: 10.1021/acs.jmedchem.8b00951. Epub 2018 Aug 23.

PMID:
30067909
3.

Metabolic Interplay between Astrocytes and Neurons Regulates Endocannabinoid Action.

Viader A, Blankman JL, Zhong P, Liu X, Schlosburg JE, Joslyn CM, Liu QS, Tomarchio AJ, Lichtman AH, Selley DE, Sim-Selley LJ, Cravatt BF.

Cell Rep. 2015 Aug 4;12(5):798-808. doi: 10.1016/j.celrep.2015.06.075. Epub 2015 Jul 23.

4.

ABHD6 blockade exerts antiepileptic activity in PTZ-induced seizures and in spontaneous seizures in R6/2 mice.

Naydenov AV, Horne EA, Cheah CS, Swinney K, Hsu KL, Cao JK, Marrs W, Blankman JL, Tu S, Cherry AE, Fung S, Wen A, Li W, Saporito MS, Selley DE, Cravatt BF, Oakley JC, Stella N.

Neuron. 2014 Jul 16;83(2):361-371. doi: 10.1016/j.neuron.2014.06.030.

5.

The serine hydrolase ABHD6 Is a critical regulator of the metabolic syndrome.

Thomas G, Betters JL, Lord CC, Brown AL, Marshall S, Ferguson D, Sawyer J, Davis MA, Melchior JT, Blume LC, Howlett AC, Ivanova PT, Milne SB, Myers DS, Mrak I, Leber V, Heier C, Taschler U, Blankman JL, Cravatt BF, Lee RG, Crooke RM, Graham MJ, Zimmermann R, Brown HA, Brown JM.

Cell Rep. 2013 Oct 31;5(2):508-20. doi: 10.1016/j.celrep.2013.08.047. Epub 2013 Oct 3.

6.

Two novel mutations in ABHD12: expansion of the mutation spectrum in PHARC and assessment of their functional effects.

Chen DH, Naydenov A, Blankman JL, Mefford HC, Davis M, Sul Y, Barloon AS, Bonkowski E, Wolff J, Matsushita M, Smith C, Cravatt BF, Mackie K, Raskind WH, Stella N, Bird TD.

Hum Mutat. 2013 Dec;34(12):1672-8. doi: 10.1002/humu.22437. Epub 2013 Oct 2.

7.

Chemical probes of endocannabinoid metabolism.

Blankman JL, Cravatt BF.

Pharmacol Rev. 2013 Mar 19;65(2):849-71. doi: 10.1124/pr.112.006387. Print 2013 Apr. Review.

8.

ABHD12 controls brain lysophosphatidylserine pathways that are deregulated in a murine model of the neurodegenerative disease PHARC.

Blankman JL, Long JZ, Trauger SA, Siuzdak G, Cravatt BF.

Proc Natl Acad Sci U S A. 2013 Jan 22;110(4):1500-5. doi: 10.1073/pnas.1217121110. Epub 2013 Jan 7.

9.

Endocannabinoid hydrolysis generates brain prostaglandins that promote neuroinflammation.

Nomura DK, Morrison BE, Blankman JL, Long JZ, Kinsey SG, Marcondes MC, Ward AM, Hahn YK, Lichtman AH, Conti B, Cravatt BF.

Science. 2011 Nov 11;334(6057):809-13. doi: 10.1126/science.1209200. Epub 2011 Oct 20.

10.

Alterations of endocannabinoid signaling, synaptic plasticity, learning, and memory in monoacylglycerol lipase knock-out mice.

Pan B, Wang W, Zhong P, Blankman JL, Cravatt BF, Liu QS.

J Neurosci. 2011 Sep 21;31(38):13420-30. doi: 10.1523/JNEUROSCI.2075-11.2011.

11.

Genetic deletion of monoacylglycerol lipase alters endocannabinoid-mediated retrograde synaptic depression in the cerebellum.

Zhong P, Pan B, Gao XP, Blankman JL, Cravatt BF, Liu QS.

J Physiol. 2011 Oct 15;589(Pt 20):4847-55. doi: 10.1113/jphysiol.2011.215509. Epub 2011 Sep 12.

12.

COX-2 and fatty acid amide hydrolase can regulate the time course of depolarization-induced suppression of excitation.

Straiker A, Wager-Miller J, Hu SS, Blankman JL, Cravatt BF, Mackie K.

Br J Pharmacol. 2011 Nov;164(6):1672-83. doi: 10.1111/j.1476-5381.2011.01486.x.

13.

The fatty acid amide hydrolase (FAAH) inhibitor PF-3845 acts in the nervous system to reverse LPS-induced tactile allodynia in mice.

Booker L, Kinsey SG, Abdullah RA, Blankman JL, Long JZ, Ezzili C, Boger DL, Cravatt BF, Lichtman AH.

Br J Pharmacol. 2012 Apr;165(8):2485-96. doi: 10.1111/j.1476-5381.2011.01445.x.

14.

Mechanistic and pharmacological characterization of PF-04457845: a highly potent and selective fatty acid amide hydrolase inhibitor that reduces inflammatory and noninflammatory pain.

Ahn K, Smith SE, Liimatta MB, Beidler D, Sadagopan N, Dudley DT, Young T, Wren P, Zhang Y, Swaney S, Van Becelaere K, Blankman JL, Nomura DK, Bhattachar SN, Stiff C, Nomanbhoy TK, Weerapana E, Johnson DS, Cravatt BF.

J Pharmacol Exp Ther. 2011 Jul;338(1):114-24. doi: 10.1124/jpet.111.180257. Epub 2011 Apr 19.

15.

Inhibitor of fatty acid amide hydrolase normalizes cardiovascular function in hypertension without adverse metabolic effects.

Godlewski G, Alapafuja SO, Bátkai S, Nikas SP, Cinar R, Offertáler L, Osei-Hyiaman D, Liu J, Mukhopadhyay B, Harvey-White J, Tam J, Pacak K, Blankman JL, Cravatt BF, Makriyannis A, Kunos G.

Chem Biol. 2010 Nov 24;17(11):1256-66. doi: 10.1016/j.chembiol.2010.08.013.

16.

Superfamily-wide portrait of serine hydrolase inhibition achieved by library-versus-library screening.

Bachovchin DA, Ji T, Li W, Simon GM, Blankman JL, Adibekian A, Hoover H, Niessen S, Cravatt BF.

Proc Natl Acad Sci U S A. 2010 Dec 7;107(49):20941-6. doi: 10.1073/pnas.1011663107. Epub 2010 Nov 17.

17.

Endocannabinoid overload.

Lichtman AH, Blankman JL, Cravatt BF.

Mol Pharmacol. 2010 Dec;78(6):993-5. doi: 10.1124/mol.110.069427. Epub 2010 Oct 15. Review.

18.

Chronic monoacylglycerol lipase blockade causes functional antagonism of the endocannabinoid system.

Schlosburg JE, Blankman JL, Long JZ, Nomura DK, Pan B, Kinsey SG, Nguyen PT, Ramesh D, Booker L, Burston JJ, Thomas EA, Selley DE, Sim-Selley LJ, Liu QS, Lichtman AH, Cravatt BF.

Nat Neurosci. 2010 Sep;13(9):1113-9. doi: 10.1038/nn.2616. Epub 2010 Aug 22.

19.

The serine hydrolase ABHD6 controls the accumulation and efficacy of 2-AG at cannabinoid receptors.

Marrs WR, Blankman JL, Horne EA, Thomazeau A, Lin YH, Coy J, Bodor AL, Muccioli GG, Hu SS, Woodruff G, Fung S, Lafourcade M, Alexander JP, Long JZ, Li W, Xu C, Möller T, Mackie K, Manzoni OJ, Cravatt BF, Stella N.

Nat Neurosci. 2010 Aug;13(8):951-7. doi: 10.1038/nn.2601. Epub 2010 Jul 25.

20.

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.

21.

Activation of the endocannabinoid system by organophosphorus nerve agents.

Nomura DK, Blankman JL, Simon GM, Fujioka K, Issa RS, Ward AM, Cravatt BF, Casida JE.

Nat Chem Biol. 2008 Jun;4(6):373-8. doi: 10.1038/nchembio.86. Epub 2008 Apr 27.

22.
23.

A functional proteomic strategy to discover inhibitors for uncharacterized hydrolases.

Li W, Blankman JL, Cravatt BF.

J Am Chem Soc. 2007 Aug 8;129(31):9594-5. Epub 2007 Jul 13. No abstract available.

PMID:
17629278

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