Structure-function relationships in estrogen receptors and the characterization of novel selective estrogen receptor modulators with unique pharmacological profiles.
This article summarizes recent research on the development of estrogen receptor alpha (ER alpha) and estrogen receptor beta (ER beta) 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 ER alpha versus ER beta 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.
Katzenellenbogen
B S
BS
Department of Molecular and Integrative Physiology, University of Illinois and College of Medicine, Urbana 61801, USA. katzenel@life.uiuc.edu
Sun
J
J
Harrington
W R
WR
Kraichely
D M
DM
Ganessunker
D
D
Katzenellenbogen
J A
JA
D000818:Animals; D015195:Drug Design; D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D005260:Female; D006801:Humans; D011960:Receptors, Estrogen / Q000187:drug effects / Q000502:physiology*; D020845:Selective Estrogen Receptor Modulators / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D011960:Receptors, Estrogen; D020845:Selective Estrogen Receptor Modulators