CCL: Call for Papers - Estrogen Receptor Symposium
- From: "Veer Shanmugasundaram"
- Subject: CCL: Call for Papers - Estrogen Receptor Symposium
- Date: Fri, 3 Mar 2006 19:01:39 -0500
Sent to CCL by: "Veer Shanmugasundaram" [Veerabahu.Shanmugasundaram
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
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.
Veer Shanmugasundaram, Ph.D
Computer-Assisted Drug Discovery,
Pfizer Global Research & Development,
2800 Plymouth Road,
Ann Arbor, MI 48105.
Neil Raheja, Ph.D
Pfizer Global Research & Development
Ann Arbor, MI 48105