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oai:www.ideals.illinois.edu:2142/84106 2023-07-11 col_2142_5131 col_2142_14789 com_2142_5130 com_2142_14788 com_2142_8903

153 p. Katzenellenbogen, John A. Rodriguez, Alice Lambert 2015-09-25T22:12:57Z 2015-09-25T22:12:57Z 10000-01-01 2003 2003 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. Made available in DSpace on 2015-09-25T22:12:57Z (GMT). No. of bitstreams: 2 license.txt: 4848 bytes, checksum: 96035ab3f5e1c23cc7138a224ce498bd (MD5) 3086167.pdf: 6111801 bytes, checksum: cc0e2301b1799ea0568998ed58aa3d5d (MD5) Previous issue date: 2003 Embargo set by: Seth Robbins for item 85387 Lift date: Forever Reason: Restricted to the U of I community idenfinitely during batch ingest of legacy ETDs Restricted to the U of I community idenfinitely during batch ingest of legacy ETDs U of I Only Thesis (Ph.D.)--University of Illinois at Urbana-Champaign, 2003. http://hdl.handle.net/2142/84106 (MiAaPQ)AAI3086167 eng Biology, Molecular I. The Development of Estrogen Receptor Coactivator Binding Inhibitors. II. Investigations Into the Binding Modes of Ligands Selective for Estrogen Receptor Alpha text Chemistry Chemistry University of Illinois at Urbana-Champaign Dissertation Ph.D.