|CCL 06.09.10 ACS Meeting, Symposium on Estrogen Receptor Ligand Binding Domain (LBD), San Francisco, CA|
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Date: Sat Mar 4 11:45:19 2006
Subject: 06.09.10 ACS Meeting, Symposium on Estrogen Receptor Ligand Binding Domain (LBD), San Francisco, CA
Venue : 232nd National Fall ACS Meeting, San Francisco, CA Dates : September 10th - 14th, 2006 Sponsored by : COMP Division Ligand-dependent activation and inactivation of transcription by nuclear hormone receptors are mediated by the recruitment of co-activators and/or co-repressors by the receptor. Receptor agonists promote co-activator binding while antagonists block co-activator binding or promote co-repressor binding thereby affecting transcriptional activity. At a molecular level, in the estrogen receptor, these mechanistic events have been explained to an extent by the solution of several estrogen receptor ligand binding domain (LBD) agonist and antagonist crystal structures. In the diethylstilbestrol (DES) agonist complex structure, the co-activator peptide binds to a hydrophobic groove on the surface of the LBD, which is promoted by a conformation of the LBD where the helix 12 is tucked over the binding pocket. In the 4-hydroxytamoxifen (OHT) antagonist structure, the side chain of OHT projects out of the ligand binding pocket, which promotes a conformation of the LBD that results in helix 12 blocking the coactivator recognition groove. However, ligands that are smaller in size (that do not have the OHT sidechain) also vary in functional activities as reported by results from several recent publications. Investigations into ER-subtype selective modulators (alpha vs beta) using structure-based methods have also been described in the literature. We plan to organize a mini-symposium that would bring together a diverse group of researchers and scientists at the 232nd National Fall ACS Meeting, San Francisco, CA, who have thought about and applied structure-based methods to the evaluation and development of selective and/or non-selective estrogen receptor modulators as well as selective and/or non-selective estrogen receptor subtype modulators. This symposium will be sponsored by the COMP division of the American Chemical Society. Symposium: Structure-Based Design & Development of Estrogen Receptor Modulators Venue : 232nd National Fall ACS Meeting, San Francisco, CA Dates : September 10th - 14th, 2006 Sponsored by : COMP Division Co-chairs : Veer Shanmugasundaram & Neil Raheja, Pfizer Global Research & Development, Ann Arbor, MI Please submit your abstracts for this symposium using OASYS http://oasys.acs.org/acs/232nm/comp/papers/index.cgi The deadline for submitting abstracts is April 25, 2006. Thank you, Veer. ---- Veer Shanmugasundaram, Ph.D Computer-Assisted Drug Discovery, Pfizer Global Research & Development, 2800 Plymouth Road, Ann Arbor, MI 48105. Tel:(734)622-7131 Fax:(734)622-2782 Email:Veerabahu.Shanmugasundaram[#]pfizer.com Neil Raheja, Ph.D Medicinal Chemistry, Pfizer Global Research & Development Ann Arbor, MI 48105 Tel: (734)622-2305 Fax:(734)622-3107 Email: Neil.Raheja[#]pfizer.comNOTE THAT E-MAIL ADDRESSES HAVE BEEN MODIFIED!!!
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