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Curr Med Chem

Title:		Free fatty acids-sensing G protein-coupled receptors in drug targeting and therapeutics
Author(s):		Yonezawa T; Kurata R; Yoshida K; Murayama MA; Cui X; Hasegawa A;
Address:		"Department of Molecular and Experimental Medicine, The Scripps Research Institute, La Jolla, California 92037, USA.. yonet2301@yahoo.co.jp"
Journal Title:		Curr Med Chem
Year:		2013
Volume:		20
Issue:		31
Page Number:		3855 - 3871
DOI:		10.2174/09298673113209990168
ISSN/ISBN:		1875-533X (Electronic) 0929-8673 (Linking)
Abstract:		"G protein-coupled receptor (GPCR) (also known as seven-transmembrane domain receptor) superfamily represents the largest protein family in the human genome. These receptors respond to various physiological ligands such as photons, odors, pheromones, hormones, ions, and small molecules including amines, amino acids to large peptides and steroids. Thus, GPCRs are involved in many diseases and the target of around half of all conventional drugs. The physiological roles of free fatty acids (FFAs), in particular, long-chain FFAs, are important for the development of many metabolic disease including obesity, diabetes, and atherosclerosis. In the past half decade, deorphanization of several GPCRs has revealed that GPR40, GPR41, GPR43, GPR84 and GPR120 sense concentration of extracellular FFAs with various carbon chain lengths. GPR40 and GPR120 are activated by medium- and long-chain FFAs. GPR84 is activated by medium- chain, but not long-chain, FFAs. GPR41 and GPR43 are activated by short-chain FFAs. GPR40 is highly expressed in pancreatic beta cells and plays a crucial role in FFAs-induced insulin secretion. GPR120 is mainly expressed in enteroendocrine cells and plays an important role for FFAs-induced glucagon-like peptide-1. GPR43 is abundant in leukocytes and adipose tissue, whilst GPR41 is highly expressed in adipose tissue, the pancreas and leukocytes. GPR84 is expressed in leukocytes and monocyte/macrophage. This review aims to shed light on the physiological roles and development of drugs targeting these receptors"
Keywords:		"Adipose Tissue/metabolism Animals Brain/metabolism Breast Neoplasms/metabolism Drug Therapy Fatty Acids, Nonesterified/*metabolism Female Gene Targeting Humans Intestinal Mucosa/metabolism Receptors, G-Protein-Coupled/*metabolism Taste Buds/metabolism;"
Notes:		"MedlineYonezawa, Tomo Kurata, Riho Yoshida, Kaori Murayama, Masanori A Cui, Xiaofeng Hasegawa, Akihiko eng Research Support, Non-U.S. Gov't Review United Arab Emirates 2013/07/19 Curr Med Chem. 2013; 20(31):3855-71. doi: 10.2174/09298673113209990168"