Pharmacologic study of C-terminal fragments of frog skin calcitonin gene-related peptide.
 

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09-23-08 08:01 AM
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Pharmacologic study of C-terminal fragments of frog skin calcitonin gene-related peptide.
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Pharmacologic study of C-terminal fragments of frog skin calcitonin gene-related peptide.

Peptides. 2008 Jul;29(7):1150-6

Authors: Ladram A, Besn&#xE9; I, Breton L, de Lacharri&#xE8;re O, Nicolas P, Amiche M

The calcitonin gene-related peptide from the skin of the frog Phyllomedusa bicolor (pbCGRP) is a 37-residue neuropeptide that differs from human alpha CGRP (halphaCGRP) at 16 positions. The affinities of the C-terminal fragments of pbCGRP and halphaCGRP were evaluated in SK-N-MC cells: pbCGRP(8-37) (K(i)=0.2nM) and pbCGRP(27-37) (K(i)=95nM) were, respectively, 3 times and 20 times more potent than the human fragments halphaCGRP(8-37) and halphaCGRP(27-37). Their antagonistic potencies were measured in SK-N-MC and Col 29 cells, and the rat vas deferens. pbCGRP(8-37) inhibited the halphaCGRP-stimulated production of cAMP by SK-N-MC and Col 29 cells 3 to 4 times more strongly than halphaCGRP(8-37). Thus pbCGRP(8-37) is the most potent CGRP-1 competitive antagonist of all the natural sequences reported to date. pbCGRP(27-37) was also as potent as [D(31), A(34), F(35)] halphaCGRP(27-37), a prototypic antagonist analog derived from structure-activity relationship studies of halphaCGRP(8-37).

PMID: 18395938 [PubMed - indexed for MEDLINE]