TY - JOUR
T1 - Structure-function relationships in estrogen receptors and the characterization of novel selective estrogen receptor modulators with unique pharmacological profiles
AU - Katzenellenbogen, Benita S.
AU - Sun, Jun
AU - Harrington, William R.
AU - Kraichely, Dennis M.
AU - Ganessunker, Deshanie
AU - Katzenellenbogen, John A.
PY - 2001
Y1 - 2001
N2 - 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.
AB - 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.
KW - Coactivators
KW - ERα
KW - ERβ
KW - SERMs
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U2 - 10.1111/j.1749-6632.2001.tb03998.x
DO - 10.1111/j.1749-6632.2001.tb03998.x
M3 - Article
C2 - 11795381
AN - SCOPUS:0035680322
SN - 0077-8923
VL - 949
SP - 6
EP - 15
JO - Annals of the New York Academy of Sciences
JF - Annals of the New York Academy of Sciences
ER -