Discovery of 1-amino-4-phenylcyclohexane-1-carboxylic acid and its influence on agonist selectivity between human melanocortin-4 and -1 receptors in linear pentapeptides.

Xin-Jie Chu,David Bartkovitz,Waleed Danho,Joseph Swistok,Adrian Wai-Hing Cheung,Grazyna Kurylko,Karen Rowan,Mitch Yeon,Lucia Franco,Lida Qi,Li Chen,Keith Yagaloff

Bioorganic & Medicinal Chemistry Letters（2006）

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摘要

A design and synthesis of cis-Apc as new histidine surrogate and its incorporation into linear pentapeptides (Penta-cis-Apc-DPhe-Arg-Trp-Gly-NH2) and related analogs leading to potent and selective hMC4R agonists are reported.

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