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 :
A series of MT-II related cyclic peptides, based on potent but non-selective hMC4R agonist (Penta-c[Asp-His6-DPhe7-Arg8-Trp9-Lys]-NH2) was prepared in which His6 residue was systematically substituted. Two of the most interesting peptides identified in this study are Penta-c[Asp-5-ClAtc-DPhe-Arg-Trp-Lys]-NH2 and Penta-c[Asp-5-ClAtc-DPhe-Cit-Trp-Lys]-NH2 which are potent hMC4R agonists and are either inactive or weak partial agonists (not tested for their antagonist activities) in hMC1R, hMC3R and hMC5R agonist assays.
