Determination of the Binding Mode of Thienopyrimidinedione Antagonists to the Human Gonadotropin Releasing Hormone Receptor Using Structure−Activity Relationships, Site-Directed Mutagenesis, and Homology Modeling
Author:
Affiliation:
1. Departments of Endocrinology and Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, California 92130
Publisher
American Chemical Society (ACS)
Subject
Drug Discovery,Molecular Medicine
Link
https://pubs.acs.org/doi/pdf/10.1021/jm060580w
Reference35 articles.
1. Fink, G. Gonadotropin secretion and its control.The Physiology ofReproduction; Raven Press: New York, 1988; pp 1349−1377.
2. Gonadotropin-Releasing Hormone Receptors
3. Lunenfeld, B.GnRH Analogues: The State of the Art at the Millennium; The Parthenon Publishing Group: New York, 1999.
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4. Progress in Structure Based Drug Design for G Protein-Coupled Receptors;Journal of Medicinal Chemistry;2011-06-15
5. Discovery of Sodium R-(+)-4-{2-[5-(2-Fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (Elagolix), a Potent and Orally Available Nonpeptide Antagonist of the Human Gonadotropin-Releasing Hormone Receptor;Journal of Medicinal Chemistry;2008-11-12
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