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Structure‐Function Relationships in Estrogen Receptors and the Characterization of Novel Selective Estrogen Receptor Modulators with Unique Pharmacological Profiles
Author(s) -
KATZENELLENBOGEN BENITA S.,
SUN JUN,
HARRINGTON WILLIAM R.,
KRAICHELY DENNIS M.,
GANESSUNKER DESHANIE,
KATZENELLENBOGEN JOHN A.
Publication year - 2001
Publication title -
annals of the new york academy of sciences
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.712
H-Index - 248
eISSN - 1749-6632
pISSN - 0077-8923
DOI - 10.1111/j.1749-6632.2001.tb03998.x
Subject(s) - estrogen receptor , estrogen receptor beta , estrogen , estrogen receptor alpha , receptor , selective estrogen receptor modulator , estrogen related receptor gamma , alpha (finance) , estrogen related receptor alpha , endocrinology , medicine , chemistry , pharmacology , biology , bioinformatics , breast cancer , cancer , construct validity , nursing , patient satisfaction
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.