β-Turn secondary structure and melanocortin ligands

Erica M. Haslach, Jay W. Schaub, Carrie Haskell-Luevano

Research output: Contribution to journalArticle

7 Scopus citations

Abstract

The melanocortin pathway has emerged during this past decade as an important target area for the discovery and development of therapeutic agents related to obesity and type 2 diabetes. This peptide-G-protein coupled receptor (GPCR) pathway has evolved from peptide-based ligands to small molecules possessing a variety of different molecular scaffolds. Herein, we summarize the originating hypothesis of the importance of the reverse β-turn secondary structure for agonist ligand potency at the melanocortin receptors and how that information was utilized for the discovery of small molecules based upon this type of turn structure.

Original languageEnglish (US)
Pages (from-to)952-958
Number of pages7
JournalBioorganic and Medicinal Chemistry
Volume17
Issue number3
DOIs
StatePublished - Feb 1 2009

Keywords

  • Diabetes
  • MC4R
  • Melanocortin
  • Melanocortin receptors
  • Melanotropin
  • Obesity

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