Peptoid−peptide hybrids as potent novel melanocortin receptor ligands

Kruijtzer, J.A.W., Nijenhuis, W.A.J., Wanders, N., Gispen, W.H., Liskamp, R.M.J. and Adan, R.A.H. (2005) Peptoid−peptide hybrids as potent novel melanocortin receptor ligands. Journal of Medicinal Chemistry, 48(13), pp. 4224-4230. (doi:10.1021/jm0490033)

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Abstract

All possible peptoid−peptide hybrids of an MC4 receptor agonist were synthesized and investigated on cells expressing different melanocortin (MC) receptor subtypes and for rat grooming behavior. In general, receptor selectivity remained while affinity and potency were decreased. The length of the functional group of Trp was more important for MC3 and MC5 than for MC4 receptor binding. In general, the potency of the peptoid−peptide hybrids to increase rat excessive grooming behavior correlated well with MC4 receptor pharmacology.

Item Type:Articles
Status:Published
Refereed:Yes
Glasgow Author(s) Enlighten ID:Liskamp, Professor Robert
Authors: Kruijtzer, J.A.W., Nijenhuis, W.A.J., Wanders, N., Gispen, W.H., Liskamp, R.M.J., and Adan, R.A.H.
College/School:College of Science and Engineering > School of Chemistry
Journal Name:Journal of Medicinal Chemistry
ISSN:0022-2623
ISSN (Online):1520-4804

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