Elsevier

Neuropeptides

Volume 31, Issue 6, December 1997, Pages 565-571
Neuropeptides

Characterization of the binding of MSH-B, HP-228, GHRP-6 and 153N-6 to the human melanocortin receptor subtypes

https://doi.org/10.1016/S0143-4179(97)90002-0Get rights and content

Abstract

We determined the binding affinities of the MSH analogues MSH-B, HP-228 and 153N-6 and of the enkephalin analogue GHRP-6 on a single eukaryotic cell line transiently expressing the human MC1, MC3, MC4 and MC5 receptors. Moreover, we tested the binding and cAMP response of MSH-B in comparison with α-MSH on murine B16 melanoma cells. Our results indicate that MSH-B has a potency similar to that of α-MSH and that these two peptides induce similar cAMP responses in murine B16 melanoma cells. HP-228 has its highest affinity for the MC1 receptor. For the other receptors, it has slightly higher affinity for the MC5 receptor than for the MC3 and MC4 receptors. 153N-6 was found to be selective for the MC1 receptor. GHRP-6 was found to bind to the MC1 and the MC5 receptors despite its low structural homology with α-MSH. [D-Lys3]GHRP-6 bound to all the four MC receptors with similar affinities. The structurally related Met-enkephalin and the functionally related GHRH, as well as LHRH and somatostatin-14 did not bind to these MC receptors. The low affinity of the GH-releasing/enkephalin peptides may indicate that they do not interact with the MC receptors at pharmacologically relevant concentrations.

References (36)

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