Approaches to the rational design of selective melanocortin receptor antagonists

Victor J. Hruby, Minying Cai, Joel Nyberg, Dhanasekaran Muthu

Research output: Contribution to journalReview article

6 Scopus citations

Abstract

Introduction: When establishing the physiological roles of specific receptors in normal and disease states, it is critical to have selective antagonist ligands for each receptor in a receptor system with several subtypes. The melanocortin receptors have five subtypes referred to as the melanocortin 1 receptor, melanocortin 2 receptor, melanocortin 3 receptor, melanocortin 4 receptor and melanocortin 5 receptor, and they are of critical importance for many aspects of human health and disease. Areas covered: This article reviews the current efforts to design selective antagonistic ligands for the five human melanocortin receptors summarizing the currently published orthosteric and allosteric antagonists for each of these receptors. Expert opinion: Though there has been progress, there are still few drugs available that address the many significant biological activities and diseases that are associated with these receptors, which is possibly due to the lack of receptor selectivity that these designed ligands are currently showing. The authors believe that further studies into the antagonists' 3D conformational and topographical properties in addition to future mutagenesis studies will provide greater insight into these ligands which could play a role in the treatment of various diseases in the future.

Original languageEnglish (US)
Pages (from-to)543-557
Number of pages15
JournalExpert Opinion on Drug Discovery
Volume6
Issue number5
DOIs
StatePublished - May 1 2011

Keywords

  • allosteric antagonist
  • melanocortin receptors
  • orthosteric antagonists
  • receptor antagonists

ASJC Scopus subject areas

  • Drug Discovery

Fingerprint Dive into the research topics of 'Approaches to the rational design of selective melanocortin receptor antagonists'. Together they form a unique fingerprint.

  • Cite this