Design of novel melanotropin agonists and antagonists with high potency and selectivity for human melanocortin receptors

Minying Cai, Alexander V. Mayorov, Jinfa Ying, Magda Stankova, Dev Trivedi, Chris Cabello, Victor J. Hruby

Research output: Contribution to journalArticle

27 Scopus citations

Abstract

α-MSH and γ-MSH are the natural endogenous hormones for the human melanocortin-1, 3, 4 and 5 receptors (hMC1R, hMC3R, hMC4R and hMC5R). These and more potent, stable and prolonged acting analogues such as NDP-α-MSH, MT-II and SHU-9119 are not very receptor selective. To develop potent and selective agonist and antagonist ligands for the melanocortin receptors we have used state-of-the-art biophysical studies, computational chemistry, and design of conformational and topographical constraints with novel templates.

Original languageEnglish (US)
Pages (from-to)1481-1485
Number of pages5
JournalPeptides
Volume26
Issue number8
DOIs
StatePublished - Aug 1 2005

Keywords

  • Conformation constraints
  • Cyclic melanotropins
  • Melanocortin receptor pharmacophores
  • Melanocortin receptors
  • Melanotropins
  • Receptor selective melanotropin agonists
  • Receptor selective melanotropin antagonists
  • Structure-biological activity relationships

ASJC Scopus subject areas

  • Biochemistry
  • Physiology
  • Endocrinology
  • Cellular and Molecular Neuroscience

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