Ontology highlight
ABSTRACT:
SUBMITTER: Mayorov AV
PROVIDER: S-EPMC3041174 | biostudies-literature | 2010 Oct
REPOSITORIES: biostudies-literature
Mayorov Alexander V AV Cai Minying M Palmer Erin S ES Liu Zhihua Z Cain James P JP Vagner Josef J Trivedi Dev D Hruby Victor J VJ
Peptides 20100803 10
A novel hybrid melanocortin pharmacophore was designed based on the pharmacophores of the agouti-signaling protein (ASIP), an endogenous melanocortin antagonist, and α-melanocyte-stimulating hormone (α-MSH), an endogenous melanocortin agonist. The designed hybrid ASIP/MSH pharmacophore was explored in monomeric cyclic, and cyclodimeric templates. The monomeric cyclic disulfide series yielded peptides with hMC3R-selective non-competitive binding affinities. The direct on-resin peptide lactam cycl ...[more]