Literature DB >> 20005104

The first synthetic agonists of FFA2: Discovery and SAR of phenylacetamides as allosteric modulators.

Yingcai Wang1, Xianyun Jiao, Frank Kayser, Jiwen Liu, Zhongyu Wang, Malgorzata Wanska, Joanne Greenberg, Jennifer Weiszmann, Hongfei Ge, Hui Tian, Simon Wong, Ralf Schwandner, Taeweon Lee, Yang Li.   

Abstract

Free fatty acid receptor 2 (FFA2) is a G-protein coupled receptor for which only short-chain fatty acids (SCFAs) have been reported as endogenous ligands. We describe the discovery and optimization of phenylacetamides as allosteric agonists of FFA2. These novel ligands can suppress adipocyte lipolysis in vitro and reduce plasma FFA levels in vivo, suggesting that these allosteric modulators can serve as pharmacological tools for exploring the potential function of FFA2 in various disease conditions. Copyright 2009 Elsevier Ltd. All rights reserved.

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Year:  2009        PMID: 20005104     DOI: 10.1016/j.bmcl.2009.11.112

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


  34 in total

1.  Extracellular loop 2 of the free fatty acid receptor 2 mediates allosterism of a phenylacetamide ago-allosteric modulator.

Authors:  Nicola J Smith; Richard J Ward; Leigh A Stoddart; Brian D Hudson; Evi Kostenis; Trond Ulven; Joanne C Morris; Christian Tränkle; Irina G Tikhonova; David R Adams; Graeme Milligan
Journal:  Mol Pharmacol       Date:  2011-04-15       Impact factor: 4.436

Review 2.  Role of Short Chain Fatty Acid Receptors in Intestinal Physiology and Pathophysiology.

Authors:  Medha Priyadarshini; Kumar U Kotlo; Pradeep K Dudeja; Brian T Layden
Journal:  Compr Physiol       Date:  2018-06-18       Impact factor: 9.090

Review 3.  Neutrophil Signaling That Challenges Dogmata of G Protein-Coupled Receptor Regulated Functions.

Authors:  Claes Dahlgren; André Holdfeldt; Simon Lind; Jonas Mårtensson; Michael Gabl; Lena Björkman; Martina Sundqvist; Huamei Forsman
Journal:  ACS Pharmacol Transl Sci       Date:  2020-03-11

4.  An Acetate-Specific GPCR, FFAR2, Regulates Insulin Secretion.

Authors:  Medha Priyadarshini; Stephanie R Villa; Miles Fuller; Barton Wicksteed; Charles R Mackay; Thierry Alquier; Vincent Poitout; Helena Mancebo; Raghavendra G Mirmira; Annette Gilchrist; Brian T Layden
Journal:  Mol Endocrinol       Date:  2015-06-15

Review 5.  The therapeutic potential of GPR43: a novel role in modulating metabolic health.

Authors:  Lauren M Cornall; Michael L Mathai; Deanne H Hryciw; Andrew J McAinch
Journal:  Cell Mol Life Sci       Date:  2013-07-14       Impact factor: 9.261

Review 6.  SCFA Receptors in Pancreatic β Cells: Novel Diabetes Targets?

Authors:  Medha Priyadarshini; Barton Wicksteed; Gary E Schiltz; Annette Gilchrist; Brian T Layden
Journal:  Trends Endocrinol Metab       Date:  2016-04-15       Impact factor: 12.015

Review 7.  G protein-coupled receptors for energy metabolites as new therapeutic targets.

Authors:  Clara C Blad; Cong Tang; Stefan Offermanns
Journal:  Nat Rev Drug Discov       Date:  2012-07-13       Impact factor: 84.694

Review 8.  Allosteric Modulation of Class A GPCRs: Targets, Agents, and Emerging Concepts.

Authors:  Eric A Wold; Jianping Chen; Kathryn A Cunningham; Jia Zhou
Journal:  J Med Chem       Date:  2018-08-28       Impact factor: 7.446

9.  Gut microbiota-derived propionate reduces cancer cell proliferation in the liver.

Authors:  L B Bindels; P Porporato; E M Dewulf; J Verrax; A M Neyrinck; J C Martin; K P Scott; P Buc Calderon; O Feron; G G Muccioli; P Sonveaux; P D Cani; N M Delzenne
Journal:  Br J Cancer       Date:  2012-09-13       Impact factor: 7.640

10.  Short-chain free fatty acid receptors FFA2/GPR43 and FFA3/GPR41 as new potential therapeutic targets.

Authors:  Trond Ulven
Journal:  Front Endocrinol (Lausanne)       Date:  2012-10-02       Impact factor: 5.555

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