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