Files in this item
Files | Description | Format |
---|---|---|
application/pdf ![]() ![]() | (no description provided) |
Description
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 |
Discipline: | Chemistry |
Degree Granting Institution: | University of Illinois at Urbana-Champaign |
Degree: | Ph.D. |
Genre: | Dissertation |
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 |
Type: | Text |
Language: | English |
Description: | 153 p. Thesis (Ph.D.)--University of Illinois at Urbana-Champaign, 2003. |
URI: | http://hdl.handle.net/2142/84106 |
Other Identifier(s): | (MiAaPQ)AAI3086167 |
Date Available in IDEALS: | 2015-09-25 |
Date Deposited: | 2003 |
This item appears in the following Collection(s)
-
Dissertations and Theses - Chemistry
-
Graduate Dissertations and Theses at Illinois
Graduate Theses and Dissertations at Illinois