4.5 Article

Recent developments in the discovery of FFA1 receptor agonists as novel oral treatment for type 2 diabetes mellitus

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 14, 页码 2991-3000

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.05.019

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Type 2 diabetes; Oral antidiabetics; GPR40; FFA1; GPCRs

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Despite the availability of established medication for treatment of type 2 diabetes mellitus (T2DM) there still remains a significant unmet need for new effective, oral antidiabetic agents that improve glycemic control while maintaining an excellent safety profile. In this regard the FFA1 receptor has emerged as an attractive target in recent years. Activation of the FFA1 receptor has been shown to not only amplify glucose induced insulin secretion from pancreatic beta cells but also to stimulate incretin secretion from intestinal endocrine cells. The current review highlights on the latest developments and clinical data from evolving research on the potential of FFA1 agonists as effective treatment for T2DM. (C) 2014 Published by Elsevier Ltd. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/3.0/).

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