Ontology highlight
ABSTRACT:
SUBMITTER: Qu H
PROVIDER: S-EPMC2775485 | biostudies-literature | 2009 Jun
REPOSITORIES: biostudies-literature
Qu Hongchang H Cai Minying M Mayorov Alexander V AV Grieco Paolo P Zingsheim Morgan M Trivedi Dev D Hruby Victor J VJ
Journal of medicinal chemistry 20090601 12
A new series of melanotropin analogues with His or Arg residues in the core pharmacophores of MTII, SHU9119, and Ac-NDP-gamma-MSH-NH(2) replaced by Pro or trans-/cis-4-guanidinyl-Pro derivatives were designed and synthesized to introduce selectivity toward the human melanocortin 4 receptor (hMC4R). Analogues 1, 2, 3, 6, 7, 8 were found to be hMC4R selective. Second messenger studies have demonstrated that analogues 1 and 2 are insurmountable inhibitors of MTII agonist activity at the hMC4R. Mole ...[more]