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Endocrinology, Vol 117, 801-805, Copyright © 1985 by Endocrine Society


ARTICLES

Conformational requirements for activity of salmon calcitonin

DM Findlay, VP Michelangeli, TJ Martin, RC Orlowski and JK Seyler

A series of deletion-substitution analogs of salmon calcitonin (SCT) have been prepared containing combinations of a glycine substitution in position 8 and deletions of serine-2 and tyrosine-22. Biological activity of the analogs with respect to native SCT were determined in the rat hypocalcemic assay and by studying stimulation of cAMP formation and competition for binding of 125I-labeled SCT in T47 D human breast cancer cells. It was found that each of the analogs retained full potency, irrespective of the means of assessment. It is suggested that conservation of the alpha-helical region of SCT, along with the overall tertiary structure, are more important for peptide potency than chain length per se.


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J. Pharmacol. Exp. Ther.Home page
L. J. Suva, M. S. Flannery, M. P. Caulfield, D. M. Findlay, H. Jüppner, S. R. Goldring, M. Rosenblatt, and M. Chorev
Design, Synthesis and Utility of Novel Benzophenone-Containing Calcitonin Analogs for Photoaffinity Labeling the Calcitonin Receptor
J. Pharmacol. Exp. Ther., November 1, 1997; 283(2): 876 - 884.
[Abstract] [Full Text]




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