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Science 25 May 1984:
Vol. 224. no. 4651, pp. 889 - 891
DOI: 10.1126/science.6326264
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Articles

Science, Vol 224, Issue 4651, 889-891
Copyright © 1984 by American Association for the Advancement of Science

articles

Synthetic competitive antagonists of corticotropin-releasing factor: effect on ACTH secretion in the rat

J Rivier, C Rivier, and W Vale

Polypeptide analogs of the known members of the corticotropin-releasing factor (CRF) family were synthesized and tested in vitro and in vivo for enhanced potency or competitive antagonism. Predictive methods and physicochemical measurements had suggested an internal secondary alpha-helical conformation spanning about 25 residues for at least three members of the CRF family. Maximization of alpha-helix-forming potential by amino acid substitutions from the native known sequences (rat/human and ovine CRF, sauvagine, and carp and sucker urotensin 1) led to the synthesis of an analog that was found to be more than twice as potent as either of the parent peptides in vitro. In contrast, certain amino-terminally shortened fragments, such as alpha-helical CRF or ovine CRF residues 8 to 41, 9 to 41, and 10 to 41, were found to be competitive inhibitors in vitro. Selected antagonists were examined and also found to be active in vivo.


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Corticotropin-Releasing Factor Increases Dihydropyridine- and Neurotoxin-Resistant Calcium Currents in Neurons of the Central Amygdala.
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