The agouti-related protein decapeptide (Yc[CRFFNAFC]Y) possesses agonist activity at the murine melanocortin-1 receptor

Carrie Haskell-Luevano, Eileen K. Monck, Y. P. Wan, Anzeela M. Schentrup

Research output: Contribution to journalArticlepeer-review

26 Scopus citations

Abstract

Agouti-related protein (AGRP) is a naturally occurring antagonist of the brain melanocortin receptors (MC3R and MC4R) and is physiologically implicated as participating in feeding behavior and energy homeostasis. The human AGRP decapeptide Yc[CRFFNAFC]Y has been previously reported as binding to the human MC3 and MC4 receptors and antagonizing the MC4 receptor. We have synthesized this decapeptide and pharmacologically characterized it at the murine melanocortin receptors and found it to possess MC4R antagonist activity (pA2 = 6.8) and, unexpectedly, MC1R agonist activity (EC50 = 2.89 μM). This study characterizes the first AGRP-based peptide agonist at the melanocortin receptors. Copyright (C) 2000 Elsevier Science Inc.

Original languageEnglish (US)
Pages (from-to)683-689
Number of pages7
JournalPeptides
Volume21
Issue number5
DOIs
StatePublished - May 2000

Bibliographical note

Funding Information:
This work has been funded by the Howard Hughes Medical Institute Research Resources Program, University of Florida. C.H.-L. is a recipient of a Burroughs Wellcome fund Career Award in the Biomedical Sciences.

Keywords

  • Agouti-related protein
  • MC1R
  • MC4R
  • Melanocortin
  • Melanotropin
  • Obesity
  • α-Melanocyte stimulating hormone

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