Cravatt, Benjamin - Department of Cell Biology, Scripps Research Institute

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Cravatt, Benjamin - Department of Cell Biology, Scripps Research Institute

Technology watch proteolysis through the eyes
Global Mapping of the Topography and Magnitude of Proteolytic
72 nature chemical biology | VOL 7 | FEBRUARY 2011 | www.nature.com/naturechemicalbiology news & views
Supplemental Experimental Procedures Cell Culture and Induction of Apoptosis
The development and application of methods for activity-based protein profiling
Proteomics and genomics A chemo-centric view of proteomics and genomics
INTRODUCTION NATURAL LIPIDS HAVE RECENTLY BEEN PROPOSED TO
Short communication Assessment of anandamide's pharmacological effects in mice deficient of
Analytical platforms for activity-based protein profiling exploiting the versatility of chemistry for functional proteomics
Activity-based protein profiling for the functional annotation of enzymes
Activity-Based Probes That Target Functional Subclasses of Phospholipases in Proteomes
Discovery of an exceptionally potent and selective class of fatty acid amide hydrolase inhibitors enlisting proteome-wide
and a HexNAc residue, suggesting that the glycan in the m/z 966.02
Research article Introduction
nature methods | VOL.5 NO.10 | OCTOBER 2008 | 859 research highlights
1. Prepare 200g of each protein sample in SDS-page loading buffer. 2. Load sample, flanked by prestained molecular weight markers onto a 10% acrylamide gel,
Identification of protein pheromones that promote aggressive behaviour
Chemistry & Biology Discovery and Characterization of a
Fatty acid amide hydrolase as a potential therapeutic target for the treatment of pain and CNS disorders
170 nature chemical biology | VOL 6 | MARCH 2010 | www.nature.com/naturechemicalbiology research highlights
Targeted Disruption of the PME-1 Gene Causes Loss of Demethylated PP2A and Perinatal Lethality in Mice
Natural Products Chemistry DOI: 10.1002/anie.200500900
Monoacylglycerol Lipase Regulates a Fatty Acid Network that
Rapid Communication Fatty Acid Amide Hydrolase, the Degradative
Autosomal Ichthyosis with Hypotrichosis Syndrome Displays Low Matriptase Proteolytic Activity and Is Phenocopied in
News & ANAlysis 5ISSN 1756-8919Future Med. Chem. (2011) 3(1), 5810.4155/FMC.10.284 2011 Future Science Ltd
Cravatt-lab Cell Fractionation Protocol [M. M. Dix, 2008] Prior to collecting conditioned media (CM), change cells to serum-free (SF) media at
Enrichment Tags for Enhanced-Resolution Profiling of the Polar Metabolome Erin E. Carlson and Benjamin F. Cravatt*
Fatty acid amide hydrolase: an emerging therapeutic target in the endocannabinoid system
Maternal PPAR protects nursing neonates by suppressing the production
1. Pan, Y. et al. Nat. Chem. Biol. 6, 708714 (2008). 2. Hille, B. Ion Channels of Excitable Membranes 3rd
A Second Mammalian N-Myristoyltransferase*
2010NatureAmerica,Inc.Allrightsreserved. nature neurOSCIenCe VOLUME 13 | NUMBER 8 | AUGUST 2010 951
Chemistry & Biology Characterization of Monoacylglycerol Lipase
Exceptionally potent inhibitors of fatty acid amide hydrolase: The enzyme responsible for degradation
The recent developments described above have made OBOC library screening
Large-scale profiling of protein palmitoylation
pubs.acs.org/jmcr XXXX American Chemical Society J. Med. Chem. XXXX, XXX, 000000 A
Novel Mechanistic Class of Fatty Acid Amide Hydrolase Inhibitors with Remarkable Selectivity
Reduced cellular expression and activity of the P129T mutant of human fatty acid amide
pubs.acs.org/jmc Published on Web 01/25/2010 r 2010 American Chemical Society 1830 J. Med. Chem. 2010, 53, 18301842
A Suite of Activity-Based Probes for Human Cytochrome P450 Aaron T. Wright, Joongyu D. Song, and Benjamin F. Cravatt*
Functional disassociation of the central and peripheral fatty acid amide signaling systems
Inhibition of Fatty-Acid Amide Hydrolase Accelerates Acquisition and Extinction Rates in a Spatial Memory Task
Fatty Acid Amide Hydrolase Competitively Degrades Bioactive Amides and Esters through a Nonconventional Catalytic Mechanism
Attenuation of Experimental Autoimmune Hepatitis by Exogenous and Endogenous Cannabinoids
Food Intake Regulates Oleoylethanolamide Formation and Degradation in the Proximal Small Intestine*
Optimization of Activity-Based Probes for Proteomic Profiling of Histone Deacetylase Complexes
Subscriber access provided by SCRIPPS RSRCH INST Journal of the American Chemical Society is published by the American Chemical
The cloned rat hydrolytic enzyme responsible for the breakdown of anandamide also catalyzes its formation via the condensation of
Bioorganic &Medicinal Chemistry Letters 8 (1998) 613-618 BIOORGANIC &
As the human genome project nears completion, biological research is entering a new era in which experimental focus will
Effect of Oleamide on Sleep and Its Relationship to Blood Pressure, Body Temperature, and Locomotor Activity in Rats
A missense mutation in human fatty acid amide hydrolase associated with problem drug use
Enzyme activity profiles of the secreted and membrane proteome that depict cancer
Increased Seizure Susceptibility and Proconvulsant Activity of Anandamide in Mice Lacking Fatty Acid Amide Hydrolase
COMPARATIVE ANALYSIS OF FATTY ACID AMIDE HYDROLASE AND CB1 CANNABINOID RECEPTOR EXPRESSION IN THE MOUSE BRAIN
Lipopolysaccharide Induces Anandamide Synthesis in Macrophages via CD14/MAPK/Phosphoinositide 3-Kinase/NF-B Independently of
Copyright 2004 by the American Society for Biochemistry and Molecular Biology, Inc. This article is available online at http://www.jlr.org Journal of Lipid Research Volume 45, 2004 757
Mice lacking fatty acid amide hydrolase exhibit a cannabinoid receptor-mediated phenotypic hypoalgesia
Reversible Inhibitors of Fatty Acid Amide Hydrolase That Promote Analgesia: Evidence for an Unprecedented
Microarray Platform for Profiling Enzyme Activities in Complex Proteomes Stephan A. Sieber, Tony S. Mondala, Steven R. Head, and Benjamin F. Cravatt*
Copyright 2005 by the American Society for Biochemistry and Molecular Biology, Inc. 342 Journal of Lipid Research Volume 46, 2005 This article is available online at http://www.jlr.org
Discovery of a Potent, Selective, and Efficacious Class of Reversible r-Ketoheterocycle Inhibitors of Fatty Acid Amide Hydrolase Effective as
Conversion of Acetaminophen to the Bioactive N-Acylphenolamine AM404 via Fatty Acid Amide Hydrolase-dependent Arachidonic Acid
Supplementary Methods Genotyping of NAPE-PLD(+/+), (+/-), and (-/-) mice by Southern blot and PCR.
Endocannabinoid Biosynthesis Proceeding through Glycerophospho-N-acyl Ethanolamine and a Role
A FAAH-Regulated Class of N-Acyl Taurines That Activates TRP Ion Channels Alan Saghatelian, Michele K. McKinney, Michael Bandell, Ardem Patapoutian, and Benjamin F. Cravatt*
Carcinoma and stromal enzyme activity profiles associated with breast tumor growth in vivo
Enzyme Classification Class Assignment of Sequence-Unrelated
Exploration of a fundamental substituent effect of a-ketoheterocycle enzyme inhibitors: Potent and selective inhibitors of fatty acid amide hydrolase
Fatty Acid Amide Hydrolase Determines Anandamide-induced Cell Death in the Liver*
A Functional Proteomic Strategy to Discover Inhibitors for Uncharacterized Weiwei Li, Jacqueline L. Blankman, and Benjamin F. Cravatt*
MOL #59030 1 Monoacyl glycerol lipase (MGL) limits the duration of
doi:10.1152/ajpheart.00107.2005 289:533-541, 2005. First published Apr 8, 2005;Am J Physiol Heart Circ Physiol
Fatty Acid Amide Hydrolase Substrate Specicity Dale L. Boger,a,c,
Disparate proteome reactivity profiles of carbon electrophiles
In Situ trans Ligands of CD22 Identified by Glycan-Protein Photocross-linking-enabled
Preservation of Striatal Cannabinoid CB1 Receptor Function Correlates with the Antianxiety Effects of Fatty Acid Amide
Characterization of mice lacking candidate N-acyl ethanolamine biosynthetic enzymes provides evidence for multiple pathways that
Regulation of Inflammatory Pain by Inhibition of Fatty Acid Amide HydrolaseS
Oxime esters as selective, covalent inhibitors of the serine hydrolase retinoblastoma-binding protein 9 (RBBP9)
RBBP9: A tumor-associated serine hydrolase activity required for pancreatic neoplasia
Dual blockade of FAAH and MAGL identifies behavioral processes regulated by endocannabinoid
Blockade of Endocannabinoid-Degrading Enzymes Attenuates Neuropathic Pain
JPET #158162 Blockade of 2-AG hydrolysis by selective monoacylglycerol lipase inhibitor JZL184
Binding and Inactivation Mechanism of a Humanized Fatty Acid Amide Hydrolase by r-Ketoheterocycle Inhibitors
Comparative Assessment of Large-Scale Proteomic Studies of Apoptotic Proteolysis
Benzothiophene piperazine and piperidine urea inhibitors of fatty acid amide hydrolase (FAAH)
Activity-based Proteomics of Enzyme Superfamilies: Serine
Identification of selective inhibitors of uncharacterized enzymes by high-throughput screening with fluorescent
Cellular/Molecular Localization of the Endocannabinoid-Degrading Enzyme
Ranking the selectivity of PubChem screening hits by activity-based protein profiling: MMP13 as a case study
Selective blockade of 2-arachidonoylglycerol hydrolysis produces cannabinoid behavioral effects
Selectivity of inhibitors of endocannabinoid biosynthesis evaluated by activity-based protein profiling
Cell Surface Proteomics Identifies Molecules Functionally Linked to Tumor Cell Intravasation*S
Proteomes take the electrophilic bait Thomas Kodadek
HEMOSTASIS, THROMBOSIS, AND VASCULAR BIOLOGY Regulation of tumor necrosis factor receptor-1 and the IKK-NF-B pathway by
2008NaturePublishingGrouphttp://www.nature.com/naturechemicalbiology Activation of the endocannabinoid system by
Localization of N-Acyl Phosphatidylethanolamine Phospholipase
Anandamide inhibits metabolism and physiological actions of 2-arachidonoylglycerol in the striatum
Brief Communications Enzymatic Machinery for Endocannabinoid Biosynthesis
Activity-Based Protein Profiling: From
Of the many fascinating discoveries made by genome-sequencing projects, perhaps none is more provocative than the prediction that
Chemistry & Biology Chemical Proteomic Probes for Profiling
Tailored Glycoproteomics and Glycan Site Mapping Using Saccharide-Selective Bioorthogonal Probes
doi:10.1152/ajpheart.00373.2007 293:909-918, 2007. First published Apr 13, 2007;Am J Physiol Heart Circ Physiol
c u r r e n t s Journal of Proteome Research Vol. 6, No. 6, 2007 2049 2007 American Chemical Society
ANALYTICAL CURRENTS J U N E 1 , 2 0 0 7 / A N A LY T I C A L C H E M I S T R Y 3 9 5 3
Potent and Selective r-Ketoheterocycle-Based Inhibitors of the Anandamide and Oleamide Catabolizing Enzyme, Fatty Acid Amide Hydrolase
Noxious compounds activate TRPA1 ion channels through covalent modification of cysteines
Role of Endocannabinoids in Alcohol Consumption and Intoxication: Studies of Mice Lacking Fatty Acid Amide
Chemoselective probes for metabolite enrichment and profiling
Endocannabinoid Metabolism in the Absence of Fatty Acid Amide Hydrolase (FAAH): Discovery of Phosphorylcholine Derivatives of N-Acyl Ethanolamines
The Putative Endocannabinoid Transport Blocker LY2183240 Is a Potent Inhibitor of FAAH and Several Other Brain Serine
Structure-Based Design of a FAAH Variant That Discriminates between the N-Acyl Ethanolamine and Taurine Families of Signaling Lipids
Bioorganic & Medicinal Chemistry Letters 9 (1999) 265-270 BIOORGANIC &
Activity-based Protein Profiling Implicates Urokinase Activation as a Key Step in Human Fibrosarcoma Intravasation*
Inactivation of N-Acyl Phosphatidylethanolamine Phospholipase D Reveals Multiple Mechanisms for the Biosynthesis of Endocannabinoids
Proteomic profiling of metalloprotease activities with cocktails of active-site probes
et al. show3, amputation of the fin in adult zebrafishprovidesasuitablemodelforstudying
Open Access Available online http://arthritis-research.com/content/8/1/R23
Increased ethanol consumption and preference and decreased ethanol sensitivity in female FAAH knockout mice
Fatty Acid Amide Hydrolase ( / ) Mice Exhibit an Increased Sensitivity to the Disruptive Effects of Anandamide or
Fax +41 61 306 12 34 E-Mail karger@karger.ch
A brain detoxifying enzyme for organophosphorus nerve poisons
Annu. Rev. Biochem. 2005. 74:41132 doi: 10.1146/annurev.biochem.74.082803.133450
Synergistic Interactions between Cannabinoids and Environmental Stress in the Activation of the Central
[Cell Cycle 4:2, e82-e84, EPUB Ahead of Print: http://www.landesbioscience.com/journals/cc/abstract.php?id=1492; February 2005]; 2005 Landes Bioscience e82 Cell Cycle 2005; Vol. 4 Issue 2
Cellular/Molecular Circuitry for Associative Plasticity in the Amygdala Involves
Segregation of two endocannabinoid-hydrolyzing enzymes into pre-and postsynaptic compartments
Activity-based probes for the proteomic profiling of metalloproteases
Structural commonalities among integral membrane enzymes Michael H. Braceya
Mapping Enzyme Active Sites in Complex Proteomes Gregory C. Adam, Jonathan Burbaum, John W. Kozarich,
Recombinant Expression, Purification, and Comparative Characterization of TorsinA and Its Torsion Dystonia-Associated Variant E-TorsinA
Evidence for Distinct Roles in Catalysis for Residues of the Serine-Serine-Lysine Catalytic Triad of Fatty Acid Amide Hydrolase*S
Global strategies to integrate the proteome and metabolome Alan Saghatelian and Benjamin F Cravatt
Trifunctional Chemical Probes for the Consolidated Detection and Identification of
Chemical Strategies for Functional Proteomics* Gregory C. Adam, Erik J. Sorensen, and Benjamin F. Cravatt
Commentaries 1130 The Journal of Clinical Investigation http://www.jci.org Volume 115 Number 5 May 2005
A Second Fatty Acid Amide Hydrolase with Variable Distribution among Placental Mammals*
Structural Basis for a Disfavored Elimination Reaction in Catalytic Antibody 1D4
Supersensitivity to anandamide and enhanced endogenous cannabinoid signaling in mice
Profiling Serine Hydrolase Activities in Complex Proteomes Dana Kidd, Yongsheng Liu, and Benjamin F. Cravatt*
Research Paper Proling the specic reactivity of the proteome with non-directed
Torsin A and Its Torsion Dystonia-associated Mutant Forms Are Lumenal Glycoproteins That Exhibit Distinct Subcellular
Clarifying the Catalytic Roles of Conserved Residues in the Amidase Signature Family*
Fatty acid amide hydrolase expression in rat choroid plexus: possible role in regulation of the sleep-inducing action of oleamide
Activity-based protein profiling: The serine hydrolases Yongsheng Liu, Matthew P. Patricelli, and Benjamin F. Cravatt*
Chemical and Mutagenic Investigations of Fatty Acid Amide Hydrolase: Evidence for a Family of Serine Hydrolases with Distinct Catalytic Properties
The Endogenous Lipid Oleamide Activates Serotonin 5-HT7 Neurons in Mouse Thalamus and Hypothalamus
Conserved Chromosomal Location and Genomic Structure of Human and Mouse Fatty-Acid Amide Hydrolase Genes and
Proc. Natl. Acad. Sci. USA Vol. 95, pp. 48104815, April 1998
The Rockefeller University Press, 0021-9525/97/12/1785/8 $2.00 The Journal of Cell Biology, Volume 139, Number 7, December 29, 1997 17851792
Proc. Natl. Acad. Sci. USA Vol. 94, pp. 22382242, March 1997
Chemical Characterization of a Family of Brain Lipids That Induce Sleep Benjamin F. Cravatt; Oscar Prospero-Garcia; Gary Siuzdak; Norton B. Gilula; Steven J.
Subscriber access provided by SCRIPPS RSRCH INST The Journal of Organic Chemistry is published by the American Chemical Society. 1155
A Tandem Orthogonal Proteolysis Strategy for High-Content Chemical Anna E. Speers and Benjamin F. Cravatt*
Pharmacological Activity of Fatty Acid Amides Is Regulated, but Not Mediated, by Fatty Acid Amide Hydrolase in Vivo
Activity-Based Protein Profiling in Vivo Using a Copper(I)-Catalyzed Azide-Alkyne [3 + 2] Cycloaddition
Chemistry & Biology A Comprehensive Profile of Brain Enzymes
Oxidative Metabolism of a Fatty Acid Amide Hydrolase-Regulated Lipid, Arachidonoyltaurine
Correlation of inhibitor effects on enzyme activity and thermal stability for the integral membrane protein fatty acid amide hydrolase
Chemical Biology Meets Biological Chemistry Minireview Series* Published, JBC Papers in Press, February 10, 2010, DOI 10.1074/jbc.R110.113126
Metalloprotease Inhibitors GM6001 and TAPI-0 Inhibit the Obligate Intracellular Human Pathogen
Subscriber access provided by SCRIPPS RSRCH INST Journal of the American Chemical Society is published by the American Chemical
Assignment of Endogenous Substrates to Enzymes by Global Metabolite Profiling Alan Saghatelian, Sunia A. Trauger, Elizabeth J. Want, Edward G. Hawkins, Gary Siuzdak, and
N-Palmitoyl Glycine, a Novel Endogenous Lipid That Acts As a Modulator of Calcium Influx and Nitric Oxide Production
BioMed Central Page 1 of 11
Tandem orthogonal proteolysis-activity-based protein profiling (TOP-ABPP)--a general method for mapping
ANANDAMIDE BIOSYNTHESIS CATALYZED BY THE PHOSPHODIESTERASE GDE1 AND DETECTION OF GLYCEROPHOSPHO-N-ACYL ETHANOLAMINE PRECURSORS IN
Transcriptional regulation of the mouse fatty acid amide hydrolase gene N.S. Waleha,*, B.F. Cravattb
Immunohistochemical Description of the Endogenous Cannabinoid System in the
Comparison of Anandamide Transport in FAAH Wild-Type and Knockout Neurons: Evidence for Contributions by both FAAH and the CB1 Receptor to
Chemical Biology ()-FR182877 Is a Potent and Selective Inhibitor
Diversity of serine hydrolase activities of unchallenged and Botrytis-infected Arabidopsis thaliana
Research article 2122 TheJournalofClinicalInvestigation http://www.jci.org Volume 116 Number 8 August 2006
Mechanism-Based Profiling of Enzyme Families Michael J. Evans and Benjamin F. Cravatt*
Serine Hydrolase KIAA1363: Toxicological and Structural Features with Emphasis on Organophosphate Interactions
Activity-Based Proteomics DOI: 10.1002/anie.200603187
Closing the Gate to the Active Site EFFECT OF THE INHIBITOR METHOXYARACHIDONYL FLUOROPHOSPHONATE ON THE
Activity-based probes for proteomic profiling of histone deacetylase complexes Cleo M. Salisbury, and Benjamin F. Cravatt
ORIGINAL INVESTIGATION Evaluation of fatty acid amide hydrolase inhibition in murine
Structure-Activity Relationships of r-Ketooxazole Inhibitors of Fatty Acid Amide Hydrolase Christophe Hardouin,, Michael J. Kelso,, F. Anthony Romero,, Thomas J. Rayl,, Donmienne Leung,, Inkyu Hwang,,
Mechanistic and structural requirements for active site labeling of phosphoglycerate mutase by spiroepoxides{
Assessing Enzyme Activities Using Stable Isotope Labeling and Mass Spectrometry Patrick A. Everley1,2
Evaluation of fatty acid amides in the carrageenan-induced paw edema model
Enzymatic Pathways That Regulate Endocannabinoid Signaling in the Nervous System
Escherichia coli Signal Peptide Peptidase A Is a Serine-Lysine Protease with a Lysine Recruited to the Nonconserved Amino-Terminal Domain in the S49 Protease
Structure-guided inhibitor design for human FAAH by interspecies active site conversion
Gabriel M. Simon & Benjamin F. Cravatt are at The Skaggs Institute for Chemical Biology and
Biomarkers of Endocannabinoid System Activation in Severe Obesity
Comparative Characterization of a Wild Type and Transmembrane Domain-Deleted Fatty Acid Amide Hydrolase: Identification of the Transmembrane Domain as a
JPET 143487 Synergy between enzyme inhibitors of fatty acid amide hydrolase and cyclooxygenase in
Research Article Theme: NIDA Symposium: Drugs of Abuse: Drug Development and Cannabinoids
DOI: 10.1002/cbic.200900244 Activity-Based Probes for Monitoring Postproline Protease
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r e s e a rc h h i g h l i g h t s Fat and furious
28 Cell 140, January 8, 2010 2010 Elsevier Inc. The work of Kumar and Wigge puts
Mice Display Differential Tolerance, Dependence, and Cannabinoid Receptor Adaptation after
The biosynthesis of N-arachidonoyl dopamine (NADA), a putative endocannabinoid and endovanilloid, via conjugation of
ChemBioChem 2004, 5, 41 47 DOI: 10.1002/cbic.200300721 2004 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim 41 Chemical Strategies for Activity-Based
april 16, 2009 VOlUME 2 / NUMBEr 15 frOM thE MakErs Of aNd
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selectivity. The best compound in the series, JZL184, is a covalent inactivator that exhib-