Literature DB >> 21764305

The discovery and development of inhibitors of fatty acid amide hydrolase (FAAH).

Katerina Otrubova1, Cyrine Ezzili, Dale L Boger.   

Abstract

A summary of the discovery and advancement of inhibitors of fatty acid amide hydrolase (FAAH) is presented.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21764305      PMCID: PMC3146581          DOI: 10.1016/j.bmcl.2011.06.096

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  106 in total

1.  Activity-based protein profiling: the serine hydrolases.

Authors:  Y Liu; M P Patricelli; B F Cravatt
Journal:  Proc Natl Acad Sci U S A       Date:  1999-12-21       Impact factor: 11.205

2.  A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.

Authors:  Sonia Gattinoni; Chiara De Simone; Sabrina Dallavalle; Filomena Fezza; Raffaella Nannei; Natalia Battista; Patrizia Minetti; Gianandrea Quattrociocchi; Antonio Caprioli; Franco Borsini; Walter Cabri; Sergio Penco; Lucio Merlini; Mauro Maccarrone
Journal:  Bioorg Med Chem Lett       Date:  2010-06-15       Impact factor: 2.823

3.  Discovery of boronic acids as novel and potent inhibitors of fatty acid amide hydrolase.

Authors:  Anna Minkkilä; Susanna M Saario; Heikki Käsnänen; Jukka Leppänen; Antti Poso; Tapio Nevalainen
Journal:  J Med Chem       Date:  2008-11-27       Impact factor: 7.446

4.  Fatty acid amide hydrolase competitively degrades bioactive amides and esters through a nonconventional catalytic mechanism.

Authors:  M P Patricelli; B F Cravatt
Journal:  Biochemistry       Date:  1999-10-26       Impact factor: 3.162

5.  Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor.

Authors:  Douglas S Johnson; Cory Stiff; Scott E Lazerwith; Suzanne R Kesten; Lorraine K Fay; Mark Morris; David Beidler; Marya B Liimatta; Sarah E Smith; David T Dudley; Nalini Sadagopan; Shobha N Bhattachar; Stephen J Kesten; Tyzoon K Nomanbhoy; Benjamin F Cravatt; Kay Ahn
Journal:  ACS Med Chem Lett       Date:  2011-02-10       Impact factor: 4.345

6.  Chemical and mutagenic investigations of fatty acid amide hydrolase: evidence for a family of serine hydrolases with distinct catalytic properties.

Authors:  M P Patricelli; M A Lovato; B F Cravatt
Journal:  Biochemistry       Date:  1999-08-03       Impact factor: 3.162

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

Authors:  Lamont Booker; Steven G Kinsey; Rehab A Abdullah; Jacqueline L Blankman; Jonathan Z Long; Cyrine Ezzili; Dale L Boger; Benjamin F Cravatt; Aron H Lichtman
Journal:  Br J Pharmacol       Date:  2012-04       Impact factor: 8.739

8.  An endogenous sleep-inducing compound is a novel competitive inhibitor of fatty acid amide hydrolase.

Authors:  M P Patricelli; J E Patterson; D L Boger; B F Cravatt
Journal:  Bioorg Med Chem Lett       Date:  1998-03-17       Impact factor: 2.823

9.  Structure-activity relationships of alpha-ketooxazole inhibitors of fatty acid amide hydrolase.

Authors:  Christophe Hardouin; Michael J Kelso; F Anthony Romero; Thomas J Rayl; Donmienne Leung; Inkyu Hwang; Benjamin F Cravatt; Dale L Boger
Journal:  J Med Chem       Date:  2007-06-09       Impact factor: 7.446

10.  Blockade of endocannabinoid-degrading enzymes attenuates neuropathic pain.

Authors:  S G Kinsey; J Z Long; S T O'Neal; R A Abdullah; J L Poklis; D L Boger; B F Cravatt; A H Lichtman
Journal:  J Pharmacol Exp Ther       Date:  2009-06-05       Impact factor: 4.030

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  39 in total

Review 1.  Inhibiting the breakdown of endogenous opioids and cannabinoids to alleviate pain.

Authors:  Bernard P Roques; Marie-Claude Fournié-Zaluski; Michel Wurm
Journal:  Nat Rev Drug Discov       Date:  2012-04       Impact factor: 84.694

2.  Human CNS barrier-forming organoids with cerebrospinal fluid production.

Authors:  Laura Pellegrini; Claudia Bonfio; Jessica Chadwick; Farida Begum; Mark Skehel; Madeline A Lancaster
Journal:  Science       Date:  2020-06-11       Impact factor: 47.728

3.  O-(triazolyl)methyl carbamates as a novel and potent class of fatty acid amide hydrolase (FAAH) inhibitors.

Authors:  Giampiero Colombano; Clara Albani; Giuliana Ottonello; Alison Ribeiro; Rita Scarpelli; Glauco Tarozzo; Jennifer Daglian; Kwang-Mook Jung; Daniele Piomelli; Tiziano Bandiera
Journal:  ChemMedChem       Date:  2014-10-22       Impact factor: 3.466

4.  Design of Benzoxathiazin-3-one 1,1-Dioxides as a New Class of Irreversible Serine Hydrolase Inhibitors: Discovery of a Uniquely Selective PNPLA4 Inhibitor.

Authors:  Anne F Kornahrens; Armand B Cognetta; Daniel M Brody; Megan L Matthews; Benjamin F Cravatt; Dale L Boger
Journal:  J Am Chem Soc       Date:  2017-05-12       Impact factor: 15.419

5.  SAR studies on truxillic acid mono esters as a new class of antinociceptive agents targeting fatty acid binding proteins.

Authors:  Su Yan; Matthew W Elmes; Simon Tong; Kongzhen Hu; Monaf Awwa; Gary Y H Teng; Yunrong Jing; Matthew Freitag; Qianwen Gan; Timothy Clement; Longfei Wei; Joseph M Sweeney; Olivia M Joseph; Joyce Che; Gregory S Carbonetti; Liqun Wang; Diane M Bogdan; Jerome Falcone; Norbert Smietalo; Yuchen Zhou; Brian Ralph; Hao-Chi Hsu; Huilin Li; Robert C Rizzo; Dale G Deutsch; Martin Kaczocha; Iwao Ojima
Journal:  Eur J Med Chem       Date:  2018-05-26       Impact factor: 6.514

Review 6.  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

7.  N-Methylimidazole-catalyzed synthesis of carbamates from hydroxamic acids via the Lossen rearrangement.

Authors:  Sabesan Yoganathan; Scott J Miller
Journal:  Org Lett       Date:  2013-01-17       Impact factor: 6.005

8.  Rational design of fatty acid amide hydrolase inhibitors that act by covalently bonding to two active site residues.

Authors:  Katerina Otrubova; Monica Brown; Michael S McCormick; Gye W Han; Scott T O'Neal; Benjamin F Cravatt; Raymond C Stevens; Aron H Lichtman; Dale L Boger
Journal:  J Am Chem Soc       Date:  2013-04-12       Impact factor: 15.419

9.  Quantum mechanics/molecular mechanics modeling of fatty acid amide hydrolase reactivation distinguishes substrate from irreversible covalent inhibitors.

Authors:  Alessio Lodola; Luigi Capoferri; Silvia Rivara; Giorgio Tarzia; Daniele Piomelli; Adrian Mulholland; Marco Mor
Journal:  J Med Chem       Date:  2013-03-07       Impact factor: 7.446

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

Authors:  Laura Bertolacci; Elisa Romeo; Marina Veronesi; Paola Magotti; Clara Albani; Mauro Dionisi; Chiara Lambruschini; Rita Scarpelli; Andrea Cavalli; Marco De Vivo; Daniele Piomelli; Gianpiero Garau
Journal:  J Am Chem Soc       Date:  2012-12-21       Impact factor: 15.419

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