Ontology highlight
ABSTRACT:
SUBMITTER: Ericson MD
PROVIDER: S-EPMC5645029 | biostudies-literature | 2017 Oct
REPOSITORIES: biostudies-literature
Ericson Mark D MD Freeman Katie T KT Schnell Sathya M SM Fleming Katlyn A KA Haskell-Luevano Carrie C
Journal of medicinal chemistry 20171004 19
The melanocortin system consists of five reported receptors, agonists from the proopiomelanocortin gene transcript, and two antagonists, agouti-signaling protein (ASP) and agouti-related protein (AGRP). For both ASP and AGRP, the hypothesized Arg-Phe-Phe pharmacophores are on exposed β-hairpin loops. In this study, the Asn and Ala positions of a reported AGRP macrocyclic scaffold (c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-DPro]) were explored with 14-compound and 8-compound libraries, respectively, to gener ...[more]