2008:Mileni M, Johnson DS, Wang Z, Everdeen DS, Liimatta M, Pabst B, Bhattacharya K, Nugent RA, Kamtekar S, Cravatt BF, Ahn K, Stevens RC. (2008) Structure-guided inhibitor design for human FAAH by interspecies active site conversion. Proc Natl Acad Sci U S A. Sep 2;105(35):12820-4. [PDF] Dix MM, Simon GM, Cravatt BF. (2008) Global mapping of the topography and magnitude of proteolytic events in apoptosis. Cell. Aug 22;134(4):679-91. [PDF] [Accompanying website] [Cell Commentary] [Nature Reviews MCB Highlight] [Nature Methods Highlight] Conn EM, Madsen MA, Cravatt BF, Ruf W, Deryugina EI, Quigley JP. (2008) Cell surface proteomics identifies molecules functionally linked to tumor cell intravasation. J Biol Chem. Sep 26;283(39):26518-27. [PDF] Hoover HS, Blankman JL, Niessen S, Cravatt BF. (2008) Selectivity of inhibitors of endocannabinoid biosynthesis evaluated by activity-based protein profiling. Bioorg Med Chem Lett. Jul 2. [Epub ahead of print] [PDF] Slaymaker IM, Bracey M, Mileni M, Garfunkle J, Cravatt BF, Boger DL, Stevens RC. (2008) Correlation of inhibitor effects on enzyme activity and thermal stability for the integral membrane protein fatty acid amide hydrolase. Bioorg Med Chem Lett. Jun 28. [Epub ahead of print] Demartino JK, Garfunkle J, Hochstatter DG, Cravatt BF, Boger DL. (2008) Exploration of a fundamental substituent effect of alpha-ketoheterocycle enzyme inhibitors: Potent and selective inhibitors of fatty acid amide hydrolase. Bioorg Med Chem Lett. Jun 28. [Epub ahead of print] [PDF] Ortega-Gutieez S, Leung D, Ficarro S, Peters EC, Cravatt BF. (2008) Targeted disruption of the PME-1 gene causes loss of demethylated PP2A and perinatal lethality in mice. PLoS ONE. Jul 2;3(7):e2486. [PDF] Suarez J, Bermudez-Silva FJ, Mackie K, Ledent C, Zimmer A, Cravatt BF, de Fonseca FR. (2008) Immunohistochemical description of the endogenous cannabinoid system in the rat cerebellum and functionally related nuclei. J Comp Neurol. 509(4):400-421. [PDF]
Nomura DK, Blankman JL, Simon GM, Fujioka K, Issa RS, Ward AM, Cravatt BF, Casida JE. (2008) Activation of the endocannabinoid system by organophosphorus nerve agents. Nat Chem Biol. 4(6):373-378. [PDF] [Faculty of 1000 Review] Ahn K, McKinney MK, Cravatt BF. (2008) Enzymatic pathways that regulate endocannabinoid signaling in the nervous system. Chem Rev. 108(5):1687-1707. [PDF] Rimmerman N, Bradshaw HB, Hughes HV, Chen JS, Hu SS, McHugh D, Vefring E, Jahnsen JA, Thompson EL, Masuda K, Cravatt BF, Burstein S, Vasko MR, Prieto AL, O'Dell DK, Walker JM. (2008) N-palmitoyl glycine, a novel endogenous lipid that acts as a modulator of calcium influx and nitric oxide production in sensory neurons. Mol Pharmacol. 74(1):213-224. [PDF] Hegde VL, Hegde S, Cravatt BF, Hofseth LJ, Nagarkatti M, Nagarkatti PS. (2008) Attenuation of experimental autoimmune hepatitis by exogenous and endogenous cannabinoids: involvement of regulatory T cells. Mol Pharmacol. 74(1):20-33. [PDF] Gaultier A, Arandjelovic S, Niessen S, Overton CD, Linton MF, Fazio S, Campana WM, Cravatt BF 3rd, Gonias SL. (2008) Regulation of tumor necrosis factor receptor-1 and the IKK-NF-kappaB pathway by LDL receptor-related protein explains the antiinflammatory activity of this receptor. Blood. 111(11):5316-5325. [PDF] Cravatt BF, Wright AT, Kozarich JW. (2008) Activity-based protein profiling: from enzyme chemistry to proteomic chemistry. Annu Rev Biochem. 77:383-414. [PDF] Nakai R, Salisbury CM, Rosen H, Cravatt BF. (2008) Ranking the selectivity of PubChem screening hits by activity-based protein profiling: MMP13 as a case study. Bioorg Med Chem. Mar 8. (epub ahead of print) [PDF] Turman MV, Kingsley PJ, Rouzer CA, Cravatt BF, Marnett LJ. (2008) Oxidative metabolism of a fatty acid amide hydrolase-regulated lipid, arachidonoyltaurine. Biochemistry. Mar 1. (epub ahead of print) [PDF] Nyilas R, Dudok B, Urban GM, Mackie K, Watanabe M, Cravatt BF, Freund TF, Katona I. (2008) Enzymatic machinery for endocannabinoid biosynthesis associated with calcium stores in glutamatergic axon terminals. J Neurosci. 28(5):1058-1063. [PDF] Simon GM, Cravatt BF. (2008) Anandamide biosynthesis catalyzed by the phosphodiesterase GDE1 and detection of glycerophospho-N-acyl ethanolamine precursors in mouse brain. J Biol Chem. Jan 27. (epub ahead of print) [PDF] Salisbury CM, Cravatt BF. (2008) Optimization of activity-based probes for proteomic profiling of histone deacetylase complexes. J Am Chem Soc. 130(7):2184-2194. [PDF] Maccarrone M, Rossi S, Bari M, De Chiara V, Fezza F, Musella A, Gasperi V, Prosperetti C, Bernardi G, Finazzi-Agro A, Cravatt BF, Centonze D. (2008) Anandamide inhibits metabolism and physiological actions of 2-arachidonoylglycerol in the striatum. Nat Neurosci. 11(2):152-159. [PDF] Nomura DK, Fujioka K, Issa RS, Ward AM, Cravatt BF, Casida JE. (2008) Dual roles of brain serine hydrolase KIAA1363 in ether lipid metabolism and organophosphate detoxification. Toxicol Appl Pharmacol. Dec 3. (epub ahead of print)
Cravatt BF, Simon GM, Yates JR 3rd (2008) The biological impact of mass-spectrometry-based proteomics. Nature. 450(7172):991-1000. [PDF] Egertová, Simon GM, Cravatt BF, Elphick MR. (2008) Localization of N-acyl phosphatidylethanolamine phospholipase D (NAPE-PLD) expression in mouse brain: A new perspective on N-acylethanolamines as neural signaling molecules. J Comp Neurol. 506(4):604-615. [PDF] 2007:Chamero P, Marton TF, Logan DW, Flanagan K, Cruz JR, Saghatelian A, Cravatt BF, Stowers L. (2007) Identification of protein pheromones that promote aggressive behaviour. Nature. 450(7171):899-902. [PDF] Carlson EE, Cravatt BF. (2007) Enrichment tags for enhanced-resolution profiling of the polar metabolome. J Am Chem Soc. Dec 5. (epub ahead of print) [PDF] Ahn K, Johnson DS, Fitzgerald LR, Liimatta M, Arendse A, Stevenson T, Lund ET, Nugent RA, Nomanbhoy TK, Alexander JP, Cravatt BF. (2007) Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity. 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(2007) Maternal PPAR-gamma protects nursing neonates by suppressing the production of inflammatory milk. Genes Dev. 21(15):1895-1908. [PDF] [Faculty of 1000 Review] Li W, Blankman JL, Cravatt BF. (2007) A functional proteomic strategy to discover inhibitors for uncharacterized hydrolases. J Am Chem Soc. 129(31):9594-9595. [PDF] Everley PA, Gartner CA, Haas W, Saghatelian A, Elias JE, Cravatt BF, Zetter BR, Gygi SP. (2007) Assessing enzyme activities using stable isotope labeling and mass spectrometry. Mol Cell Proteomics. 6(10):1771-1777. [PDF] Evans MJ, Morris GM, Wu J, Olson AJ, Sorensen EJ, Cravatt BF. (2007) Mechanistic and structural requirements for active site labeling of phosphoglycerate mutase by spiroepoxides. Mol Biosyst. 3(7):495-506. [PDF] Hardouin C, Kelso MJ, Romero FA, Rayl TJ, Leung D, Hwang I, Cravatt BF, Boger DL. (2007) Structure-activity relationships of alpha-ketooxazole inhibitors of fatty acid amide hydrolase. J Med Chem. 50(14):3359-68. 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(2007) Noxious compounds activate TRPA1 ion channels through covalent modification of cysteines. Nature. 445(7127):541-545. [PDF] [Nature Commentary] [Faculty of 1000 Review] Salisbury CM, Cravatt BF. (2007) Activity-based probes for proteomic profiling of histone deacetylase complexes. Proc Natl Acad Sci U S A. 104(4):1171-1176. [PDF] [Faculty of 1000 Review] Bogyo M, Cravatt BF. (2007) Genomics and proteomics. From genes to function: advances in applications of chemical and systems biology. Curr Opin Chem Biol. 11(1):1-3. [PDF] Blednov YA, Cravatt BF, Boehm SL 2nd, Walker D, Harris RA. (2007) Role of endocannabinoids in alcohol consumption and intoxication: Studies of mice lacking fatty acid amide hydrolase. Neuropsychopharmacology. 32(7):1570-1582. [PDF] 2006:Wise LE, Shelton CC, Cravatt BF, Martin BR, Lichtman AH. (2006) Assessment of anandamide's pharmacological effects in mice deficient of both fatty acid amide hydrolase and cannabinoid CB(1) receptors. 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Varvel SA, Wise LE, Niyuhire F, Cravatt BF, Lichtman AH. (2007) Inhibition of fatty-acid amide hydrolase accelerates acquisition and extinction rates in a spatial memory task. Neuropsychopharmacology. 32(5):1032-1041. [PDF] Barglow KT, Cravatt BF. (2006) Substrate mimicry in an activity-based probe that targets the nitrilase family of enzymes. Angew Chem Int Ed Engl. 45(44):7408-7411. [PDF] [Faculty of 1000 Review] Wei BQ, Mikkelsen TS, McKinney MK, Lander ES, Cravatt BF. (2006) A second fatty acid amide hydrolase with variable distribution among placental mammals. J Biol Chem. 281(48):36569-36578. [PDF] Mulder AM, Cravatt BF. (2006) Endocannabinoid metabolism in the absence of fatty acid amide hydrolase (FAAH): Discovery of phosphorylcholine derivatives of N-acyl ethanolamines. Biochemistry. 45(38):11267-11277. [PDF] Nomura DK, Durkin KA, Chiang KP, Quistad GB, Cravatt BF, Casida JE. (2006) Serine hydrolase KIAA1363: Toxicological and structural features with emphasis on organophosphate interactions. Chem Res Toxicol. 19(9):1142-1150. [PDF] Evans MJ, Cravatt BF. (2006) Mechanism-based profiling of enzyme families. Chem Rev. 106(8):3279-3301. [PDF] Wang H, Xie H, Guo Y, Zhang H, Takahashi T, Kingsley PJ, Marnett LJ, Das SK, Cravatt BF, Dey SK. (2006) Fatty acid amide hydrolase deficiency limits early pregnancy events. J Clin Invest. 116(8):2122-2131. [PDF] Alexander JP, Cravatt BF. (2006) The putative endocannabinoid transport blocker LY2183240 is a potent inhibitor of FAAH and several other brain serine hydrolases. J Am Chem Soc. 128(30):9699-9704. [PDF] [ACS Chemical Biology Commentary] McKinney MK, Cravatt BF. (2006) Structure-based design of a FAAH variant that discriminates between the N-acyl ethanolamine and taurine families of signaling lipids. Biochemistry. 45(30):9016-9022. [PDF] Saghatelian A, McKinney MK, Bandell M, Patapoutian A, Cravatt BF. (2006) A FAAH-regulated class of N-acyl taurines that activates TRP ion channels. Biochemistry. 45(30):9007-9015. [PDF] Simon GM, Cravatt BF. (2006) Endocannabinoid biosynthesis proceeding through glycerophospho-N-acyl ethanolamine and a role for alpha/beta hydrolase 4 in this pathway. J Biol Chem. 281(36):26465-26472. [PDF] Safo PK, Cravatt BF, Regehr WG. (2006) Retrograde endocannabinoid signaling in the cerebellar cortex. Cerebellum. 5(2):134-145. Sieber SA, Cravatt BF. (2006) Analytical platforms for activity-based protein profiling - exploiting the versatility of chemistry for functional proteomics. Chem Commun (Camb). 22:2311-2319. [PDF] Madsen MA, Deryugina EI, Niessen S, Cravatt BF, Quigley JP. (2006) Activity based protein profiling implicates urokinase (uPA) activation as a key step in human fibrosarcoma intravasation. J Biol Chem. 281(23):15997-16005. [PDF] Leung D, Saghatelian A, Simon GM, Cravatt BF. (2006) Inactivation of N-acyl phosphatidylethanolamine phospholipase D reveals multiple mechanisms for the biosynthesis of endocannabinoids. Biochemistry. 45(15):4720-4726. [PDF] [Supplemental Material] Sieber SA, Niessen S, Hoover HS, Cravatt BF. (2006) Proteomic profiling of metalloprotease activities with cocktails of active-site probes. Nat Chem Biol. 2(5):274-281. [PDF] [Nature Chemical Biology Commentary] Balakrishnan A, Patel B, Sieber SA, Chen D, Pachikara N, Zhong G, Cravatt BF, Fan H. (2006) Metalloprotease inhibitors GM6001 and TAPI-0 inhibit the obligate intracellular human pathogen Chlamydia trachomatis by targeting peptide deformylase of the bacterium. J Biol Chem. 281(24):16691-16699. [PDF] Milner JM, Kevorkian L, Young DA, Jones D, Wait R, Donell ST, Barksby E, Patterson AM, Middleton J, Cravatt BF, Clark IM, Rowan AD, Cawston TE. (2006) Fibroblast activation protein alpha is expressed by chondrocytes following a pro-inflammatory stimulus and is elevated in osteoarthritis. Arthritis Res Ther. 8(1):R23. [PDF] Basavarajappa BS, Yalamanchili R, Cravatt BF, Cooper TB, Hungund BL. (2006) Increased ethanol consumption and preference and decreased ethanol sensitivity in female FAAH knockout mice. Neuropharmacology. 50(7):834-844. [PDF] Siegmund SV, Seki E, Osawa Y, Uchinami H, Cravatt BF, Schwabe RF. (2006) Fatty acid amide hydrolase determines anandamide-induced cell death in the liver. J Biol Chem. 281(15):10431-10438. [PDF] 2005:Saghatelian A, Cravatt BF. (2005) Assignment of protein function in the postgenomic era. Nat Chem Biol. 1(3):130-142. [PDF] Varvel SA, Cravatt BF, Engram AE, Lichtman AH. (2005) FAAH (-/-) mice exhibit an increased sensitivity to the disruptive effects of anandamide or oleamide in a working memory water maze task. J Pharmacol Exp Ther. 317(1):251-257. [PDF]
Want EJ, Cravatt BF, Siuzdak G. (2005) The expanding role of mass spectrometry in metabolite profiling and characterization. Chembiochem. 6(11):1941-1951. Evans MJ, Saghatelian A, Sorensen EJ, Cravatt BF (2005) Target discovery in small-molecule cell-based screens by in situ proteome reactivity profiling. Nat Biotechnol. 23(10):1303-1307. [PDF] [Nature Commentary] [C&E News Commentary] [Journal of Biomolecular Techniques Commentary] Cravatt BF. (2005) Live chemical reports from the cell surface. Chem Biol. 12(9):954-956. Drahl C, Cravatt BF, Sorensen EJ. (2005) Protein-reactive natural products. Angew Chem Int Ed Engl. 44(36):5788-5809. [PDF] Osei-Hyiaman D, Depetrillo M, Harvey-White J, Bannon AW, Cravatt BF, Kuhar MJ, Mackie K, Palkovits M, Kunos G. (2005) Cocaine- and amphetamine-related transcript peptide is involved in the orexigenic effect of endogenous anandamide. Neuroendocrinology. 81(4):273-282. Jessani N, Niessen S, Wei BQ, Nicolau M, Humphrey M, Ji Y, Han W, Noh DY, Yates JR 3rd, Jeffrey SS, Cravatt BF. (2005) A streamlined platform for high-content functional proteomics of primary human specimens. Nat Methods. 2(9):691-697. [PDF] Speers AE, Cravatt BF. (2005) A tandem orthogonal proteolysis strategy for high-content chemical proteomics. J Am Chem Soc. 127(28):10018-10019. [PDF] [Faculty of 1000 Review] Hogestatt ED, Jonsson BA, Ermund A, Andersson DA, Bjork H, Alexander JP, Cravatt BF, Basbaum AI, Zygmunt PM. (2005) Conversion of acetaminophen to the bioactive N-acyl phenolamine AM404 via fatty acid amide hydrolase-dependent arachidonic acid conjugation in the nervous system. J Biol Chem. 280(36):31405-31412. [PDF] Saghatelian A, Cravatt BF. (2005) Discovery metabolite profiling - forging functional connections between the proteome and metabolome. Life Sci. 77(14):1759-1766. Cravatt BF (2005) Kinase chemical genomics--a new rule for the exceptions. Nat Methods. 2:411-412. 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Angew Chem Int Ed Engl. 44(16):2400-2403. [PDF] [Faculty of 1000 Review] Boger DL, Miyauchi H, Du W, Hardouin C, Fecik RA, Cheng H, Hwang I, Hedrick MP, Leung D, Acevedo O, Guimaraes CRW, Jorgensen WL, CravattBF. (2005) Discovery of a potent, selective, and efficacious class of reversible alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase effective as analgesics. J Med Chem. 48(6):1849-1856. [PDF] McKinney MK, Cravatt BF. (2005) Structure and function of fatty acid amide hydrolase. Annu Rev Biochem. 74:411-432. [PDF] Patel S, Cravatt BF, Hillard CJ. (2005) Synergistic interactions between cannabinoids and environmental stress in the activation of the central amygdala. Neuropsychopharmacology. 30(3):497-507. [PDF] Leung D, Du W, Hardouin C, Cheng H, Hwang I, Cravatt BF, Boger DL. 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(2004) Functional disassociation of the central and peripheral fatty acid amide signaling systems. Proc Natl Acad Sci USA. 101(29):10821-10826. [PDF] Gulyas AI, Cravatt BF, Bracey MH, Dinh TP, Piomelli D, Boscia F, Freund TF. (2004) Segregation of two endocannabinoid-hydrolyzing enzymes into pre- and postsynaptic compartments in the rat hippocampus, cerebellum and amygdala. Eur J Neurosci. 20(2):441-458. [PDF] Lichtman AH, Leung D, Shelton C, Saghatelian A, Hardouin C, Boger D, Cravatt BF. (2004) Reversible inhibitors of fatty acid amide hydrolase that promote analgesia: evidence for an unprecedented combination of potency and selectivity. J Pharmacol Exp Ther. 311(2):441-448. [PDF] Saghatelian A, Jessani N, Joseph A, Humphrey M, Cravatt BF. (2004) Activity-based probes for the proteomic profiling of metalloproteases. Proc Natl Acad Sci USA. 101(27):10000-10005. [PDF] Ortega-Gutierrez S, Hawkins EG, Viso A, Lopez-Rodriguez ML, Cravatt BF. 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