COMP 4 |
| A large number of structures of the ligand binding domain of both the alpha and beta forms of the estrogen receptor (ER) have been published. This includes complexes with various peptides derived from co-activators or co-repressors as well as different ligands, including partial and full agonists and selective and full antagonists. This has provided insights at the molecular level into some key aspects of the pharmacology and function of the protein. This presentation will review the published structures and summarise both how far the structural results can be related to the known functions of the receptor(s) and what lessons are available for design of new compounds. Finally, I will summarise our progress in generating suitable material for structural studies of full length receptor in complex with ligand, DNA and co-activator.
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Structure-Based Design & Development of Estrogen Receptor Modulators
9:00 AM-12:35 PM, Sunday, 10 September 2006 Moscone Center -- Room 224/226, Oral
Division of Computers in Chemistry |