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Science 7 November 1980:
Vol. 210. no. 4470, pp. 656 - 658
DOI: 10.1126/science.7001627
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Articles

Science, Vol 210, Issue 4470, 656-658
Copyright © 1980 by American Association for the Advancement of Science

articles

Bioactive conformation of luteinizing hormone-releasing hormone: evidence from a conformationally constrained analog

RM Freidinger, DF Veber, DS Perlow, Brooks JR, and R Saperstein

An analog of luteinizing hormone-releasing hormone containing a gamma-lactam as a conformational constraint has been prepared with the use of a novel cyclization of a methionine sulfonium salt. The analog is more active as a luteinizing hormone-releasing hormone agonist that the parent hormone, and provides evidence for a bioactive conformation containing a beta-turn.


THIS ARTICLE HAS BEEN CITED BY OTHER ARTICLES:
Conformational Constraint of Mammalian, Chicken, and Salmon GnRHs, But Not GnRH II, Enhances Binding at Mammalian and Nonmammalian Receptors: Evidence for Preconfiguration of GnRH II.
K. D. G. Pfleger, J. Bogerd, and R. P. Millar (2002)
Mol. Endocrinol. 16, 2155-2162
   Abstract »    Full Text »    PDF »
Role of Aspartate7.32(302) of the Human Gonadotropin-Releasing Hormone Receptor in Stabilizing a High-Affinity Ligand Conformation.
B. J. Fromme, A. A. Katz, R. W. Roeske, R. P. Millar, and C. A. Flanagan (2001)
Mol. Pharmacol. 60, 1280-1287
   Abstract »    Full Text »    PDF »
Asn102 of the Gonadotropin-releasing Hormone Receptor Is a Critical Determinant of Potency for Agonists Containing C-terminal Glycinamide.
J. S. Davidson, C. A. McArdle, P. Davies, R. Elario, C. A. Flanagan, and R. P. Millar (1996)
J. Biol. Chem. 271, 15510-15514
   Abstract »    Full Text »    PDF »


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