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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

Bioorg Med Chem Lett. 2005 Nov 15;15(22):4910-4.

PMID: 16169218

Abstract:

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 agonist potency and selectivity against hMC1R in linear pentapeptides.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP827521 Phenylcyclohexane Phenylcyclohexane 827-52-1 Price
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