Design of cyclic and other templates for potent and selective peptide α-MSH analogues

Selena Fung, Victor J. Hruby

Research output: Contribution to journalReview article

33 Scopus citations

Abstract

For over three decades, the design of linear peptide ligands often has incorporated cyclic constraints to improve potency, receptor selectivity, proteolytic stability and biodistribution. Its importance has been so well established that modern day schemes for ligand-based drug design often start with cyclization of linear peptides to rigidify peptide structure, to limit its conformational possibilities, and to find key pharmacophore elements in three-dimensional space. In the past several years, cyclic constraints have been used to develop ligands with improved efficacy, binding affinity, biostability and receptor selectivity for α-melanocyte-stimulating hormone (α-MSH). Furthermore, potent cyclic α-MSH analogues, such as MT-II and SHU-9119, have made structure-activity relationship studies and molecular modeling more useful for creating new three-dimensional, topographical pharmacophore templates.

Original languageEnglish (US)
Pages (from-to)352-358
Number of pages7
JournalCurrent Opinion in Chemical Biology
Volume9
Issue number4
DOIs
StatePublished - Aug 1 2005

ASJC Scopus subject areas

  • Analytical Chemistry
  • Biochemistry

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