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Title:I. The Development of Estrogen Receptor Coactivator Binding Inhibitors. II. Investigations Into the Binding Modes of Ligands Selective for Estrogen Receptor Alpha
Author(s):Rodriguez, Alice Lambert
Doctoral Committee Chair(s):Katzenellenbogen, John A.
Department / Program:Chemistry
Degree Granting Institution:University of Illinois at Urbana-Champaign
Subject(s):Biology, Molecular
Abstract:Our laboratory has previously discovered that certain heterocycles show high binding affinity and selectivity for ERalpha. In order to design more potent and selective derivatives, a better understanding of how they bind to the receptor is needed. Using a comparative binding analysis method and molecular modeling, we were able to assess the binding mode of a furan agonist and antagonist. As an agonist, the furan binds to the receptor with the C(2) phenol acting as the A-ring in most cases. As an antagonist, the furan binds with the C(5) phenol acting as the A-ring mimic and the basic side chain extending back into the pocket in a similar fashion to known antagonists. The preparation of various mono and bisphenolic furan analogs in conjunction with molecular modeling assisted in confirming these assertions.
Issue Date:2003
Description:153 p.
Thesis (Ph.D.)--University of Illinois at Urbana-Champaign, 2003.
Other Identifier(s):(MiAaPQ)AAI3086167
Date Available in IDEALS:2015-09-25
Date Deposited:2003

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