| Literature DB >> 12895657 |
Diane M Ignar1, John L Andrews, Marilyn Jansen, Michelle M Eilert, Heather M Pink, Peiyuan Lin, Ronald G Sherrill, Jerzy R Szewczyk, James G Conway.
Abstract
The lack of specific pharmacological tools has impeded the evaluation of the role of each melanocortin receptor (MCR) subtype in the myriad physiological effects of melanocortins. 154N-5 is an octapeptide (MFRdWFKPV-NH(2)) that was first identified as an MC1R antagonist in Xenopus melanophores [J. Biol. Chem. 269 (1994) 29846]. In this manuscript, we show that 154N-5 is a specific agonist for human and murine MC1R. The peptide has negligible activity at MC3R and MC4R and is 25-fold less potent and a weak agonist at MC5R. 154N-5 was tested in both a cellular and an animal model of tumor necrosis factor-alpha (TNF-alpha) secretion. The inhibitory efficacy of 154N-5 on TNF-alpha secretion in both models was similar to the nonselective agonist NDP-alpha-melanocyte stimulating hormone (NDP-alphaMSH), thus, we conclude that inhibition of TNF-alpha secretion by melanocortin peptides is mediated by MC1R. 154N-5 is a valuable new tool for the evaluation of specific contribution of MC1R agonism to physiological and pathological processes.Entities:
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Year: 2003 PMID： 12895657 DOI： 10.1016/s0196-9781(03)00127-x
Source DB: PubMed Journal: Peptides ISSN： 0196-9781 Impact factor: 3.750