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Structure‐Function Relationships in Estrogen Receptors and the Characterization of Novel Selective Estrogen Receptor Modulators with Unique Pharmacological Profiles

2001; Wiley; Volume: 949; Issue: 1 Linguagem: Inglês

10.1111/j.1749-6632.2001.tb03998.x

1749-6632

Benita S. Katzenellenbogen, Jun Sun, William R. Harrington, Dennis M. Kraichely, Deshanie Ganessunker, John A. Katzenellenbogen,

Inflammatory mediators and NSAID effects

A bstract : This article summarizes recent research on the development of estrogen receptor alpha (ERα) and estrogen receptor beta (ERβ) subtype‐selective ligands based on our understanding of structure‐activity relationships in these two estrogen receptors and differences in their ligand binding domains and activation function domains. The use of these ligands should enable greater understanding of the unique biologies mediated by ERα versus ERβ and may, as well, provide selective estrogen receptor modulators having unique biological and pharmacological profiles optimal for prevention and treatment of breast cancer, for menopausal hormone replacement, for prevention of osteoporosis, and for potential cardiovascular benefit.