Peptoid−Peptide Hybrids as Potent Novel Melanocortin Receptor Ligands

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 fu...

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Veröffentlicht in:	Journal of medicinal chemistry 2005-06, Vol.48 (13), p.4224-4230
Hauptverfasser:	Kruijtzer, John A. W, Nijenhuis, Wouter A. J, Wanders, Nienke, Gispen, Willem Hendrik, Liskamp, Rob M. J, Adan, Roger A. H
Format:	Artikel
Sprache:	eng
Schlagworte:	Amino Acid Sequence Amino Acid Substitution Animals Binding Sites Biological and medical sciences Injections, Intraventricular Ligands Medical sciences Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Oligopeptides - administration & dosage Oligopeptides - chemical synthesis Oligopeptides - chemistry Oligopeptides - pharmacokinetics Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Peptoids - administration & dosage Peptoids - chemical synthesis Peptoids - chemistry Peptoids - pharmacokinetics Pharmacology. Drug treatments Rats Receptor, Melanocortin, Type 3 - metabolism Receptor, Melanocortin, Type 4 - metabolism Receptors, Corticotropin - metabolism Receptors, Melanocortin - metabolism
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Zusammenfassung:	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.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm0490033