Peptides having potent antagonist and agonist bioactivities at m

Details Peptides having potent antagonist and agonist bioactivities at m Peptides having potent antagonist and agonist bioactivities at m

1995-04-10

1998-03-24

Tsang, Cecilia J.

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

Cyclic peptides

530312, 930270, C07K 700

Patent

active

057314080

ABSTRACT:
Cyclic lactam peptides, seven amino acids in length, having D-2'-naphthylalanine (D-2'-Nal) or D-para-iodo-phenylalanine D-(p-I)Phe at position 4 of the peptide provided potent and specific antagonists of the two neural melanocortin receptors and of the peripheral receptor. In particular, the peptide ##STR1## was found to be a potent antagonist of the MC3 and MC4 receptors with partial agonist activity, and a full agonist of the MC1 and MC5 receptors; the peptide ##STR2## was found to be a potent antagonist of the MC3 and MC4 receptors with partial agonist activity. Both peptides have antagonist activities in the classical frog skin bioassay for pigmentation at the MC1 receptor.

REFERENCES:
Adan et al., "Identification of antagonists for melanocortin MC.sub.3, MCb.4, and MC.sub.5 receptors." Eur. J. Pharmacol., 269, 331-338, 1994.
Johnson et al., "Coat color darkening in a dog in response to a potent melanotropic peptide." Am. J. Vet. Res.,55(11), 1593-6, 1994.
Ito et al., "Structure-Activity Correlations of Melanotropin Peptides in Model Lipids by Tryptophan Fluorescence Studies".
Biochemistry, 32(45), 12264-72, 1993.

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