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Items: 40


Inhibitory Control Deficits Associated with Upregulation of CB1R in the HIV-1 Tat Transgenic Mouse Model of Hand.

Jacobs IR, Xu C, Hermes DJ, League AF, Xu C, Nath B, Jiang W, Niphakis MJ, Cravatt BF, Mackie K, Mukhopadhyay S, Lichtman AH, Ignatowska-Jankowska BM, Fitting S.

J Neuroimmune Pharmacol. 2019 Dec;14(4):661-678. doi: 10.1007/s11481-019-09867-w. Epub 2019 Aug 1.


Quantification of In Vivo Target Engagement Using Microfluidic Activity-Based Protein Profiling.

Reardon HT, Herbst RA, Henry CL, Herbst DM, Ngo N, Cisar JS, Weber OD, Niphakis MJ, O'Neill GP.

SLAS Technol. 2019 Oct;24(5):489-498. doi: 10.1177/2472630319852303. Epub 2019 Jun 14.


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 Dec;367(3):494-508. doi: 10.1124/jpet.118.252296. Epub 2018 Oct 10.


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.


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.


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.


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.


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.


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

Owens RA, Ignatowska-Jankowska B, Mustafa M, Beardsley PM, Wiley JL, Jali A, Selley DE, Niphakis MJ, Cravatt BF, Lichtman AH.

J Pharmacol Exp Ther. 2016 Aug;358(2):306-14. doi: 10.1124/jpet.115.229492. Epub 2016 Jun 15.


Elevation of 2-AG by monoacylglycerol lipase inhibition in the visceral insular cortex interferes with anticipatory nausea in a rat model.

Limebeer CL, Rock EM, Puvanenthirarajah N, Niphakis MJ, Cravatt BF, Parker LA.

Behav Neurosci. 2016 Apr;130(2):261-6. doi: 10.1037/bne0000132.


The Selective Monoacylglycerol Lipase Inhibitor MJN110 Produces Opioid-Sparing Effects in a Mouse Neuropathic Pain Model.

Wilkerson JL, Niphakis MJ, Grim TW, Mustafa MA, Abdullah RA, Poklis JL, Dewey WL, Akbarali H, Banks ML, Wise LE, Cravatt BF, Lichtman AH.

J Pharmacol Exp Ther. 2016 Apr;357(1):145-56. doi: 10.1124/jpet.115.229971. Epub 2016 Jan 20.


Diacylglycerol lipase disinhibits VTA dopamine neurons during chronic nicotine exposure.

Buczynski MW, Herman MA, Hsu KL, Natividad LA, Irimia C, Polis IY, Pugh H, Chang JW, Niphakis MJ, Cravatt BF, Roberto M, Parsons LH.

Proc Natl Acad Sci U S A. 2016 Jan 26;113(4):1086-91. doi: 10.1073/pnas.1522672113. Epub 2016 Jan 11.


Double Dissociation of Monoacylglycerol Lipase Inhibition and CB1 Antagonism in the Central Amygdala, Basolateral Amygdala, and the Interoceptive Insular Cortex on the Affective Properties of Acute Naloxone-Precipitated Morphine Withdrawal in Rats.

Wills KL, Petrie GN, Millett G, Limebeer CL, Rock EM, Niphakis MJ, Cravatt BF, Parker LA.

Neuropsychopharmacology. 2016 Jun;41(7):1865-73. doi: 10.1038/npp.2015.356. Epub 2015 Dec 9.


Endocannabinoid regulation of nausea is mediated by 2-arachidonoylglycerol (2-AG) in the rat visceral insular cortex.

Sticht MA, Limebeer CL, Rafla BR, Abdullah RA, Poklis JL, Ho W, Niphakis MJ, Cravatt BF, Sharkey KA, Lichtman AH, Parker LA.

Neuropharmacology. 2016 Mar;102:92-102. doi: 10.1016/j.neuropharm.2015.10.039. Epub 2015 Nov 2.


Interference with acute nausea and anticipatory nausea in rats by fatty acid amide hydrolase (FAAH) inhibition through a PPARα and CB1 receptor mechanism, respectively: a double dissociation.

Rock EM, Limebeer CL, Ward JM, Cohen A, Grove K, Niphakis MJ, Cravatt BF, Parker LA.

Psychopharmacology (Berl). 2015 Oct;232(20):3841-8. doi: 10.1007/s00213-015-4050-7. Epub 2015 Aug 23.


Selective N-Hydroxyhydantoin Carbamate Inhibitors of Mammalian Serine Hydrolases.

Cognetta AB 3rd, Niphakis MJ, Lee HC, Martini ML, Hulce JJ, Cravatt BF.

Chem Biol. 2015 Jul 23;22(7):928-37. doi: 10.1016/j.chembiol.2015.05.018. Epub 2015 Jun 25.


A Global Map of Lipid-Binding Proteins and Their Ligandability in Cells.

Niphakis MJ, Lum KM, Cognetta AB 3rd, Correia BE, Ichu TA, Olucha J, Brown SJ, Kundu S, Piscitelli F, Rosen H, Cravatt BF.

Cell. 2015 Jun 18;161(7):1668-80. doi: 10.1016/j.cell.2015.05.045.


Facile synthesis of borofragments and their evaluation in activity-based protein profiling.

Adachi S, Cognetta AB 3rd, Niphakis MJ, He Z, Zajdlik A, St Denis JD, Scully CC, Cravatt BF, Yudin AK.

Chem Commun (Camb). 2015 Feb 28;51(17):3608-11. doi: 10.1039/c4cc09107h.


Δ9-tetrahydrocannabinol and endocannabinoid degradative enzyme inhibitors attenuate intracranial self-stimulation in mice.

Wiebelhaus JM, Grim TW, Owens RA, Lazenka MF, Sim-Selley LJ, Abdullah RA, Niphakis MJ, Vann RE, Cravatt BF, Wiley JL, Negus SS, Lichtman AH.

J Pharmacol Exp Ther. 2015 Feb;352(2):195-207. doi: 10.1124/jpet.114.218677. Epub 2014 Nov 14.


Effect of selective inhibition of monoacylglycerol lipase (MAGL) on acute nausea, anticipatory nausea, and vomiting in rats and Suncus murinus.

Parker LA, Niphakis MJ, Downey R, Limebeer CL, Rock EM, Sticht MA, Morris H, Abdullah RA, Lichtman AH, Cravatt BF.

Psychopharmacology (Berl). 2015 Feb;232(3):583-93. doi: 10.1007/s00213-014-3696-x. Epub 2014 Aug 3.


Mapping the protein interaction landscape for fully functionalized small-molecule probes in human cells.

Kambe T, Correia BE, Niphakis MJ, Cravatt BF.

J Am Chem Soc. 2014 Jul 30;136(30):10777-82. doi: 10.1021/ja505517t. Epub 2014 Jul 21.


Endocannabinoids modulate cortical development by configuring Slit2/Robo1 signalling.

Alpár A, Tortoriello G, Calvigioni D, Niphakis MJ, Milenkovic I, Bakker J, Cameron GA, Hanics J, Morris CV, Fuzik J, Kovacs GG, Cravatt BF, Parnavelas JG, Andrews WD, Hurd YL, Keimpema E, Harkany T.

Nat Commun. 2014 Jul 17;5:4421. doi: 10.1038/ncomms5421.


Enzyme inhibitor discovery by activity-based protein profiling.

Niphakis MJ, Cravatt BF.

Annu Rev Biochem. 2014;83:341-77. doi: 10.1146/annurev-biochem-060713-035708. Review.


Remodeling natural products: chemistry and serine hydrolase activity of a rocaglate-derived β-lactone.

Lajkiewicz NJ, Cognetta AB 3rd, Niphakis MJ, Cravatt BF, Porco JA Jr.

J Am Chem Soc. 2014 Feb 12;136(6):2659-64. doi: 10.1021/ja412431g. Epub 2014 Feb 4.


In vivo characterization of the highly selective monoacylglycerol lipase inhibitor KML29: antinociceptive activity without cannabimimetic side effects.

Ignatowska-Jankowska BM, Ghosh S, Crowe MS, Kinsey SG, Niphakis MJ, Abdullah RA, Tao Q, O' Neal ST, Walentiny DM, Wiley JL, Cravatt BF, Lichtman AH.

Br J Pharmacol. 2014 Mar;171(6):1392-407. doi: 10.1111/bph.12298.


Evaluation of NHS carbamates as a potent and selective class of endocannabinoid hydrolase inhibitors.

Niphakis MJ, Cognetta AB 3rd, Chang JW, Buczynski MW, Parsons LH, Byrne F, Burston JJ, Chapman V, Cravatt BF.

ACS Chem Neurosci. 2013 Sep 18;4(9):1322-32. doi: 10.1021/cn400116z. Epub 2013 Jun 17.


Proteome-wide reactivity profiling identifies diverse carbamate chemotypes tuned for serine hydrolase inhibition.

Chang JW, Cognetta AB 3rd, Niphakis MJ, Cravatt BF.

ACS Chem Biol. 2013 Jul 19;8(7):1590-9. doi: 10.1021/cb400261h. Epub 2013 May 23.


Determining target engagement in living systems.

Simon GM, Niphakis MJ, Cravatt BF.

Nat Chem Biol. 2013 Apr;9(4):200-5. doi: 10.1038/nchembio.1211. No abstract available.


Proteome-wide mapping of cholesterol-interacting proteins in mammalian cells.

Hulce JJ, Cognetta AB, Niphakis MJ, Tully SE, Cravatt BF.

Nat Methods. 2013 Mar;10(3):259-64. doi: 10.1038/nmeth.2368. Epub 2013 Feb 10.


Dual inhibition of endocannabinoid catabolic enzymes produces enhanced antiwithdrawal effects in morphine-dependent mice.

Ramesh D, Gamage TF, Vanuytsel T, Owens RA, Abdullah RA, Niphakis MJ, Shea-Donohue T, Cravatt BF, Lichtman AH.

Neuropsychopharmacology. 2013 May;38(6):1039-49. doi: 10.1038/npp.2012.269. Epub 2013 Jan 3.


Selective inhibitors and tailored activity probes for lipoprotein-associated phospholipase A(2).

Nagano JM, Hsu KL, Whitby LR, Niphakis MJ, Speers AE, Brown SJ, Spicer T, Fernandez-Vega V, Ferguson J, Hodder P, Srinivasan P, Gonzalez TD, Rosen H, Bahnson BJ, Cravatt BF.

Bioorg Med Chem Lett. 2013 Feb 1;23(3):839-43. doi: 10.1016/j.bmcl.2012.11.061. Epub 2012 Dec 2.


Copper-assisted palladium(II)-catalyzed direct arylation of cyclic enaminones with arylboronic acids.

Kim YW, Niphakis MJ, Georg GI.

J Org Chem. 2012 Nov 2;77(21):9496-503. doi: 10.1021/jo301531k. Epub 2012 Oct 22.


Synthesis and evaluation of the anti-proliferative and NF-κB activities of a library of simplified tylophorine analogs.

Niphakis MJ, Gay BC, Hong KH, Bleeker NP, Georg GI.

Bioorg Med Chem. 2012 Oct 1;20(19):5893-900. doi: 10.1016/j.bmc.2012.07.044. Epub 2012 Aug 3.


O-hydroxyacetamide carbamates as a highly potent and selective class of endocannabinoid hydrolase inhibitors.

Niphakis MJ, Johnson DS, Ballard TE, Stiff C, Cravatt BF.

ACS Chem Neurosci. 2012 May 16;3(5):418-26. doi: 10.1021/cn200089j. Epub 2011 Oct 10.


Highly selective inhibitors of monoacylglycerol lipase bearing a reactive group that is bioisosteric with endocannabinoid substrates.

Chang JW, Niphakis MJ, Lum KM, Cognetta AB 3rd, Wang C, Matthews ML, Niessen S, Buczynski MW, Parsons LH, Cravatt BF.

Chem Biol. 2012 May 25;19(5):579-88. doi: 10.1016/j.chembiol.2012.03.009. Epub 2012 Apr 26.


Palladium(II)-catalyzed dehydrogenative alkenylation of cyclic enaminones via the Fujiwara-Moritani reaction.

Yu YY, Niphakis MJ, Georg GI.

Org Lett. 2011 Nov 4;13(21):5932-5. doi: 10.1021/ol202677g. Epub 2011 Oct 13.


Synthesis of tylocrebrine and related phenanthroindolizidines by VOF3-mediated oxidative aryl-alkene coupling.

Niphakis MJ, Georg GI.

Org Lett. 2011 Jan 21;13(2):196-9. doi: 10.1021/ol1023954. Epub 2010 Dec 14.


Synthesis of 6- and 7-membered cyclic enaminones: scope and mechanism.

Niphakis MJ, Turunen BJ, Georg GI.

J Org Chem. 2010 Oct 15;75(20):6793-805. doi: 10.1021/jo100907u.


Total syntheses of arylindolizidine alkaloids (+)-ipalbidine and (+)-antofine.

Niphakis MJ, Georg GI.

J Org Chem. 2010 Sep 3;75(17):6019-22. doi: 10.1021/jo101051w.


Palladium(II)-catalyzed direct arylation of enaminones using organotrifluoroborates.

Ge H, Niphakis MJ, Georg GI.

J Am Chem Soc. 2008 Mar 26;130(12):3708-9. doi: 10.1021/ja710221c. Epub 2008 Mar 6.


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