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
Publication statusPublished - Aug 2005

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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
  • Endocrinology
  • Physiology
  • Cellular and Molecular Neuroscience

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