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

…, W Danho, J Swistok, AWH Cheung, G Kurylko…

文献索引：Chu, Xin-Jie; Bartkovitz, David; Danho, Waleed; Swistok, Joseph; Cheung, Adrian Wai-Hing; Kurylko, Grazyna; Rowan, Karen; Yeon, Mitch; Franco, Lucia; Qi, Lida; Chen, Li; Yagaloff, Keith Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 22 p. 4910 - 4914

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被引用次数: 9

摘要

Linear pentapeptides (Penta-cis-Apc-DPhe-Arg-Trp-Gly-NH2) containing 1-amino-4- phenylcyclohexane-1-carboxylic acid (cis-Apc) and substituted Apc are potent hMC4R agonists and they are inactive or weakly active in hMC1R, hMC3R, and hMC5R agonist assays. This study, together with our earlier report on 5-BrAtc, demonstrated the importance of replacing His6 with phenyl-containing rigid templates in achieving good hMC4R ...