Current Drug Targets

Francis J. Castellino
Kleiderer-Pezold Professor of Biochemistry
Director, W.M. Keck Center for Transgene Research
Dean Emeritus, College of Science
230 Raclin-Carmichael Hall, University of Notre Dame
Notre Dame, IN 46556


GPR40 Carboxylic Acid Receptor Family and Diabetes: A New Drug Target

Author(s): V. N. Telvekar and H. S. Kundaikar

Affiliation: Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, University of Mumbai, Matunga, Mumbai-400 019, Maharashtra, India.

Keywords: G- protein coupled receptor, tyrosine kinase receptor, orphan GPCR, GPR40 carboxylic acid family, free fatty acids, type 2 diabetes, glucose stimulated insulin secretion, oligomerisation


Type-2 diabetes is strongly linked to visceral obesity and elevated levels of circulating free fatty acids. For years this correlation of obesity to diabetes has intrigued the minds of researchers and research in this direction has led to a possible solution to this question. Human Genome project has identified nearly 150 orphan GPCRs. The reverse pharmacology approaches have identified free fatty acids as ligands for the GPR40 family of orphan receptors. This review mainly emphasizes on the role of GPR40 carboxylic acid receptor family in the development of diabetes alongwith detailed coverage of each receptor of the family. GPR40 family has provided an insight into regulation of carbohydrate and lipid metabolism in vertebrates and has further provided targets for the development of therapeutic agents useful for treating or preventing disorders such as Type-2 diabetes. This review also suggests where further research and development could be beneficial.

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Article Details

Page: [899 - 910]
Pages: 12
DOI: 10.2174/138945008785909301