Eleven amino acid glucagon-like peptide-1 receptor agonists with antidiabetic activity

…, ES Sieber-McMaster, KL Constantine…

文献索引：Mapelli, Claudio; Natarajan, Sesha I.; Meyer, Jean-Philippe; Bastos, Margarita M.; Bernatowicz, Michael S.; Lee, Ving G.; Pluscec, Jelka; Riexinger, Douglas J.; Sieber-McMaster, Ellen S.; Constantine, Keith L.; Smith-Monroy, Constance A.; Golla, Rajasree; Ma, Zhengping; Longhi, Daniel A.; Shi, Dan; Xin, Li; Taylor, Joseph R.; Koplowitz, Barry; Chi, Cecilia L.; Khanna, Ashish; Robinson, Gordon W.; Seethala, Ramakrishna; Antal-Zimanyi, Ildiko A.; Stoffel, Robert H.; Han, Songping; Whaley, Jean M.; Huang, Christine S.; Krupinski, John; Ewing, William R. Journal of Medicinal Chemistry, 2009 , vol. 52, # 23 p. 7788 - 7799

全文：HTML全文

被引用次数: 36

摘要

Glucagon-like peptide 1 (GLP-1) is a 30 or 31 amino acid peptide hormone that contributes to the physiological regulation of glucose homeostasis and food intake. Herein, we report the discovery of a novel class of 11 amino acid GLP-1 receptor agonists. These peptides consist of a structurally optimized 9-mer, which is closely related to the N-terminal 9 amino acids of GLP-1, linked to a substituted C-terminal biphenylalanine (BIP) dipeptide. SAR ...