Literature DB >> 17465724

Fatty acid receptors as new therapeutic targets for diabetes.

Geetha Vani Rayasam1, Vamshi Krishna Tulasi, Joseph Alex Davis, Vinay S Bansal.   

Abstract

G-protein-coupled receptors (GPCRs) are key regulators of several physiological functions. Their roles in cellular signal transduction have made them the target for majority of all currently prescribed drugs. Additionally, there are many orphan GPCRs that provide potential novel therapeutic targets. Several GPCRs are involved in metabolic regulation and glucose homeostasis such as GLP-1 receptor, glucagon receptor, adiponectin receptor and so on. Recently, free fatty acids (FFAs) have been demonstrated as ligands for orphan GPCRs and have been proposed to play a critical role in physiological glucose homeostasis. GPR40 and GPR120 are activated by medium and long-chain FFAs, whereas GPR41 and GPR43 can be activated by short-chain FFAs. GPR40, which is preferentially expressed in pancreatic beta-cells, mediates the majority of the effects of FFAs on insulin secretion. In this review, these findings and also critical analysis of these GPCRs as novel targets for diabetes are discussed.

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Year:  2007        PMID: 17465724     DOI: 10.1517/14728222.11.5.661

Source DB:  PubMed          Journal:  Expert Opin Ther Targets        ISSN: 1472-8222            Impact factor:   6.902


  28 in total

1.  Activation of oral trigeminal neurons by fatty acids is dependent upon intracellular calcium.

Authors:  Tian Yu; Bhavik P Shah; Dane R Hansen; MieJung Park-York; Timothy A Gilbertson
Journal:  Pflugers Arch       Date:  2012-05-30       Impact factor: 3.657

Review 2.  Seven transmembrane-spanning receptors for free fatty acids as therapeutic targets for diabetes mellitus: pharmacological, phylogenetic, and drug discovery aspects.

Authors:  Stefano Costanzi; Susanne Neumann; Marvin C Gershengorn
Journal:  J Biol Chem       Date:  2008-04-02       Impact factor: 5.157

3.  Mercaptoacetate and fatty acids exert direct and antagonistic effects on nodose neurons via GPR40 fatty acid receptors.

Authors:  Rebecca A Darling; Huan Zhao; Dallas Kinch; Ai-Jun Li; Steven M Simasko; Sue Ritter
Journal:  Am J Physiol Regul Integr Comp Physiol       Date:  2014-04-23       Impact factor: 3.619

4.  Transient receptor potential channel type M5 is essential for fat taste.

Authors:  Pin Liu; Bhavik P Shah; Stephanie Croasdell; Timothy A Gilbertson
Journal:  J Neurosci       Date:  2011-06-08       Impact factor: 6.167

5.  Discovery of the First Environment-Sensitive Fluorescent Probe for GPR120 (FFA4) Imaging.

Authors:  Jiaxiang Liu; Chengsen Tian; Tianyu Jiang; Yuqi Gao; Yubin Zhou; Minyong Li; Lupei Du
Journal:  ACS Med Chem Lett       Date:  2017-03-27       Impact factor: 4.345

6.  A novel insulinotropic mechanism of whole grain-derived γ-oryzanol via the suppression of local dopamine D2 receptor signalling in mouse islet.

Authors:  Chisayo Kozuka; Sumito Sunagawa; Rei Ueda; Moritake Higa; Yuzuru Ohshiro; Hideaki Tanaka; Chigusa Shimizu-Okabe; Chitoshi Takayama; Masayuki Matsushita; Masato Tsutsui; Shogo Ishiuchi; Masanori Nakata; Toshihiko Yada; Jun-Ichi Miyazaki; Seiichi Oyadomari; Michio Shimabukuro; Hiroaki Masuzaki
Journal:  Br J Pharmacol       Date:  2015-08-03       Impact factor: 8.739

Review 7.  Magnificent seven: roles of G protein-coupled receptors in extracellular sensing in fungi.

Authors:  Chaoyang Xue; Yen-Ping Hsueh; Joseph Heitman
Journal:  FEMS Microbiol Rev       Date:  2008-09-22       Impact factor: 16.408

8.  Structural requirements for the cytoprotective actions of mono-unsaturated fatty acids in the pancreatic beta-cell line, BRIN-BD11.

Authors:  S Dhayal; H J Welters; N G Morgan
Journal:  Br J Pharmacol       Date:  2008-02-25       Impact factor: 8.739

9.  Metabolic shifts due to long-term caloric restriction revealed in nonhuman primates.

Authors:  Serge Rezzi; François-Pierre J Martin; Dhanansayan Shanmuganayagam; Ricki J Colman; Jeremy K Nicholson; Richard Weindruch
Journal:  Exp Gerontol       Date:  2009-03-03       Impact factor: 4.032

10.  Discovery of novel agonists and antagonists of the free fatty acid receptor 1 (FFAR1) using virtual screening.

Authors:  Irina G Tikhonova; Chi Shing Sum; Susanne Neumann; Stanislav Engel; Bruce M Raaka; Stefano Costanzi; Marvin C Gershengorn
Journal:  J Med Chem       Date:  2008-01-15       Impact factor: 7.446

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