Design of novel melanocortin receptor ligands: Multiple receptors, complex pharmacology, the challenge

Victor J. Hruby; Minying Cai; James Cain; Joel Nyberg; Dev Trivedi

doi:10.1016/j.ejphar.2010.10.109

Design of novel melanocortin receptor ligands: Multiple receptors, complex pharmacology, the challenge

Victor J. Hruby
, Minying Cai
, James Cain
, Joel Nyberg
, Dev Trivedi

Research output: Contribution to journal › Review article › peer-review

18 Scopus citations

Abstract

The major pharmacophore for the melanocortin 1, 3, 4 and 5 receptors is the sequence -His-Phe-Arg-Trp-. There is a need for potent, biologically stable, receptor selective ligands, both agonists and antagonists, for these receptors. In this report we briefly examine the structural and biophysical approaches we have taken to develop selective agonist and antagonist ligands that can cross (or not) the blood brain barrier. Remaining questions and unmet needs are also discussed.

Original language	English (US)
Pages (from-to)	88-93
Number of pages	6
Journal	European Journal of Pharmacology
Volume	660
Issue number	1
DOIs	https://doi.org/10.1016/j.ejphar.2010.10.109
State	Published - Jun 11 2011

Keywords

Agonists and antagonists for MCR
Melanocortin receptor ligand SAR
Melanocortin receptor selective ligand
Orthosteric and allosteric ligand
Selective ligand for MCR

ASJC Scopus subject areas

Pharmacology

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10.1016/j.ejphar.2010.10.109

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title = "Design of novel melanocortin receptor ligands: Multiple receptors, complex pharmacology, the challenge",

abstract = "The major pharmacophore for the melanocortin 1, 3, 4 and 5 receptors is the sequence -His-Phe-Arg-Trp-. There is a need for potent, biologically stable, receptor selective ligands, both agonists and antagonists, for these receptors. In this report we briefly examine the structural and biophysical approaches we have taken to develop selective agonist and antagonist ligands that can cross (or not) the blood brain barrier. Remaining questions and unmet needs are also discussed.",

keywords = "Agonists and antagonists for MCR, Melanocortin receptor ligand SAR, Melanocortin receptor selective ligand, Orthosteric and allosteric ligand, Selective ligand for MCR",

author = "Hruby, \{Victor J.\} and Minying Cai and James Cain and Joel Nyberg and Dev Trivedi",

note = "Funding Information: We are particularly grateful to the many outstanding collaborators and colleagues who have made this research possible. Their names appear in the publications referenced here and in many other critical publications. The research was supported in part by grants from the U.S. Public Health Service . We thank Margie Colie for her help with the manuscript.",

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doi = "10.1016/j.ejphar.2010.10.109",

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AU - Hruby, Victor J.

AU - Cai, Minying

AU - Cain, James

AU - Nyberg, Joel

AU - Trivedi, Dev

N1 - Funding Information: We are particularly grateful to the many outstanding collaborators and colleagues who have made this research possible. Their names appear in the publications referenced here and in many other critical publications. The research was supported in part by grants from the U.S. Public Health Service . We thank Margie Colie for her help with the manuscript.

PY - 2011/6/11

Y1 - 2011/6/11

N2 - The major pharmacophore for the melanocortin 1, 3, 4 and 5 receptors is the sequence -His-Phe-Arg-Trp-. There is a need for potent, biologically stable, receptor selective ligands, both agonists and antagonists, for these receptors. In this report we briefly examine the structural and biophysical approaches we have taken to develop selective agonist and antagonist ligands that can cross (or not) the blood brain barrier. Remaining questions and unmet needs are also discussed.

AB - The major pharmacophore for the melanocortin 1, 3, 4 and 5 receptors is the sequence -His-Phe-Arg-Trp-. There is a need for potent, biologically stable, receptor selective ligands, both agonists and antagonists, for these receptors. In this report we briefly examine the structural and biophysical approaches we have taken to develop selective agonist and antagonist ligands that can cross (or not) the blood brain barrier. Remaining questions and unmet needs are also discussed.

KW - Agonists and antagonists for MCR

KW - Melanocortin receptor ligand SAR

KW - Melanocortin receptor selective ligand

KW - Orthosteric and allosteric ligand

KW - Selective ligand for MCR

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DO - 10.1016/j.ejphar.2010.10.109

M3 - Review article

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JF - European Journal of Pharmacology

IS - 1

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Design of novel melanocortin receptor ligands: Multiple receptors, complex pharmacology, the challenge

Abstract

Keywords

ASJC Scopus subject areas

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