Literature DB >> 23240907

A binding site for nonsteroidal anti-inflammatory drugs in fatty acid amide hydrolase.

Laura Bertolacci1, Elisa Romeo, Marina Veronesi, Paola Magotti, Clara Albani, Mauro Dionisi, Chiara Lambruschini, Rita Scarpelli, Andrea Cavalli, Marco De Vivo, Daniele Piomelli, Gianpiero Garau.   

Abstract

In addition to inhibiting the cyclooxygenase (COX)-mediated biosynthesis of prostanoids, various widely used nonsteroidal anti-inflammatory drugs (NSAIDs) enhance endocannabinoid signaling by blocking the anandamide-degrading membrane enzyme fatty acid amide hydrolase (FAAH). The X-ray structure of FAAH in complex with the NSAID carprofen, along with site-directed mutagenesis, enzyme activity assays, and NMR analysis, has revealed the molecular details of this interaction, providing information that may guide the design of dual FAAH-COX inhibitors with superior analgesic efficacy.

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Year:  2012        PMID： 23240907      PMCID： PMC3562592          DOI： 10.1021/ja308733u

Source DB:  PubMed          Journal:  J Am Chem Soc        ISSN： 0002-7863            Impact factor:   15.419


  41 in total

Review 1.  Prostanoid receptors: subtypes and signaling.

Authors:  R M Breyer; C K Bagdassarian; S A Myers; M D Breyer
Journal:  Annu Rev Pharmacol Toxicol       Date:  2001       Impact factor: 13.820

2.  Peripheral FAAH inhibition causes profound antinociception and protects against indomethacin-induced gastric lesions.

Authors:  Oscar Sasso; Rosalia Bertorelli; Tiziano Bandiera; Rita Scarpelli; Giampiero Colombano; Andrea Armirotti; Guillermo Moreno-Sanz; Angelo Reggiani; Daniele Piomelli
Journal:  Pharmacol Res       Date:  2012-03-07       Impact factor: 7.658

Review 3.  Can we conquer pain?

Authors:  Joachim Scholz; Clifford J Woolf
Journal:  Nat Neurosci       Date:  2002-11       Impact factor: 24.884

4.  Supersensitivity to anandamide and enhanced endogenous cannabinoid signaling in mice lacking fatty acid amide hydrolase.

Authors:  B F Cravatt; K Demarest; M P Patricelli; M H Bracey; D K Giang; B R Martin; A H Lichtman
Journal:  Proc Natl Acad Sci U S A       Date:  2001-07-24       Impact factor: 11.205

Review 5.  Prostaglandins and leukotrienes: advances in eicosanoid biology.

Authors:  C D Funk
Journal:  Science       Date:  2001-11-30       Impact factor: 47.728

6.  Effects of pH on the inhibition of fatty acid amidohydrolase by ibuprofen.

Authors:  S Holt; J Nilsson; R Omeir; G Tiger; C J Fowler
Journal:  Br J Pharmacol       Date:  2001-06       Impact factor: 8.739

7.  A role for endocannabinoids in indomethacin-induced spinal antinociception.

Authors:  Hans Gühring; May Hamza; Marina Sergejeva; Mehmet Ates; Carolin E Kotalla; Catherine Ledent; Kay Brune
Journal:  Eur J Pharmacol       Date:  2002-11-15       Impact factor: 4.432

8.  Structural insights into the stereochemistry of the cyclooxygenase reaction.

Authors:  J R Kiefer; J L Pawlitz; K T Moreland; R A Stegeman; W F Hood; J K Gierse; A M Stevens; D C Goodwin; S W Rowlinson; L J Marnett; W C Stallings; R G Kurumbail
Journal:  Nature       Date:  2000-05-04       Impact factor: 49.962

9.  Structural adaptations in a membrane enzyme that terminates endocannabinoid signaling.

Authors:  Michael H Bracey; Michael A Hanson; Kim R Masuda; Raymond C Stevens; Benjamin F Cravatt
Journal:  Science       Date:  2002-11-29       Impact factor: 47.728

Review 10.  Fatty acid amide hydrolase: an emerging therapeutic target in the endocannabinoid system.

Authors:  Benjamin F Cravatt; Aron H Lichtman
Journal:  Curr Opin Chem Biol       Date:  2003-08       Impact factor: 8.822
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  18 in total

1.  Combined inhibition of monoacylglycerol lipase and cyclooxygenases synergistically reduces neuropathic pain in mice.

Authors:  Molly S Crowe; Emma Leishman; Matthew L Banks; Ramesh Gujjar; Anu Mahadevan; Heather B Bradshaw; Steven G Kinsey
Journal:  Br J Pharmacol       Date:  2015-01-20       Impact factor: 8.739

Review 2.  A Double Whammy: Targeting Both Fatty Acid Amide Hydrolase (FAAH) and Cyclooxygenase (COX) To Treat Pain and Inflammation.

Authors:  Rita Scarpelli; Oscar Sasso; Daniele Piomelli
Journal:  ChemMedChem       Date:  2015-10-21       Impact factor: 3.466

3.  An insight into paracetamol and its metabolites using molecular docking and molecular dynamics simulation.

Authors:  Yuanqiang Wang; Weiwei Lin; Nan Wu; Xibing He; Junmei Wang; Zhiwei Feng; Xiang-Qun Xie
Journal:  J Mol Model       Date:  2018-08-18       Impact factor: 1.810

4.  Keys to Lipid Selection in Fatty Acid Amide Hydrolase Catalysis: Structural Flexibility, Gating Residues and Multiple Binding Pockets.

Authors:  Giulia Palermo; Inga Bauer; Pablo Campomanes; Andrea Cavalli; Andrea Armirotti; Stefania Girotto; Ursula Rothlisberger; Marco De Vivo
Journal:  PLoS Comput Biol       Date:  2015-06-25       Impact factor: 4.475

5.  Inhibition of endocannabinoid metabolism by the metabolites of ibuprofen and flurbiprofen.

Authors:  Jessica Karlsson; Christopher J Fowler
Journal:  PLoS One       Date:  2014-07-25       Impact factor: 3.240

Review 6.  Care and feeding of the endocannabinoid system: a systematic review of potential clinical interventions that upregulate the endocannabinoid system.

Authors:  John M McPartland; Geoffrey W Guy; Vincenzo Di Marzo
Journal:  PLoS One       Date:  2014-03-12       Impact factor: 3.240

7.  Interaction of the N-(3-Methylpyridin-2-yl)amide Derivatives of Flurbiprofen and Ibuprofen with FAAH: Enantiomeric Selectivity and Binding Mode.

Authors:  Jessica Karlsson; Carmine M Morgillo; Alessandro Deplano; Giovanni Smaldone; Emilia Pedone; F Javier Luque; Mona Svensson; Ettore Novellino; Cenzo Congiu; Valentina Onnis; Bruno Catalanotti; Christopher J Fowler
Journal:  PLoS One       Date:  2015-11-13       Impact factor: 3.240

8.  The Molecular Basis for Dual Fatty Acid Amide Hydrolase (FAAH)/Cyclooxygenase (COX) Inhibition.

Authors:  Giulia Palermo; Angelo D Favia; Marino Convertino; Marco De Vivo
Journal:  ChemMedChem       Date:  2015-11-23       Impact factor: 3.466

9.  Discovery of a Carbazole-Derived Lead Drug for Human African Trypanosomiasis.

Authors:  Sarah M Thomas; Andrei Purmal; Michael Pollastri; Kojo Mensa-Wilmot
Journal:  Sci Rep       Date:  2016-08-26       Impact factor: 4.379

10.  The long-acting COX-2 inhibitor mavacoxib (Trocoxil™) has anti-proliferative and pro-apoptotic effects on canine cancer cell lines and cancer stem cells in vitro.

Authors:  Lisa Y Pang; Sally A Argyle; Ayako Kamida; Katherine O'Neill Morrison; David J Argyle
Journal:  BMC Vet Res       Date:  2014-09-05       Impact factor: 2.741
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