Author/Authors :
Adrian Wai-Hing Cheung، نويسنده , , Waleed Danho، نويسنده , , Joseph Swistok، نويسنده , , Lida Qi، نويسنده , , Grazyna Kurylko، نويسنده , , Karen Rowan، نويسنده , , Mitch Yeon، نويسنده , , Lucia Franco، نويسنده , , Xin-Jie Chu، نويسنده , , Li Chen، نويسنده , , Keith Yagaloff، نويسنده ,
Abstract :
Systematic substitution of His6 residue using non-selective hMC4R pentapeptide agonist (Bu-His6-DPhe7-Arg8-Trp9-Gly10-NH2) as the template led to the identification of Bu-Atc6(2- mino etraline-2- arboxylic acid)-DPhe7-Arg8-Trp9-Gly10-NH2 which showed moderate selectivity towards hMC4R over hMC1R. Further SAR studies resulted in the discovery of Penta-5-BrAtc6-DPhe7-Arg8-Trp9-Gly10-NH2 and Penta-5-Me2NAtc6-DPhe7-Arg8-Trp9-Gly10-NH2 which are potent hMC4R agonists and are inactive in hMC1R, hMC3R and hMC5R agonist assays.
