[Estrogen receptor subtypes and the regulatory effect of receptor ligand binding on gene transcription].
This review introduces the structure, functions, tissue distribution, physiologic roles of estrogen receptor subtypes (ER alpha and ER beta) along with transcriptional activities of estrogen receptor ligands and the mechanism of the modulatory pathway and tissue specific property of selective estrogen receptor modulators (SERMs), and phytoestrogens. This article is to provide a systemic approach for increasing the selectivity of estrogenic drug and optimizing the clinically based strategy of drug design. Differences exist between ER alpha and ER beta in structure, function, tissue distribution, physiologic roles and response to ligands, as well as the regulating effect on gene transcription, which are mainly determined by different co-regulators they recruit respectively.
An
Sheng-Jun
SJ
Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing 100850.
Zhang
Yong-Xiang
YX
D000818:Animals; D004967:Estrogens / Q000494:pharmacology*; D005260:Female; D005786:Gene Expression Regulation / Q000187:drug effects*; D008024:Ligands; D008297:Male; D010937:Plant Growth Regulators / Q000494:pharmacology*; D051381:Rats; D011960:Receptors, Estrogen / Q000737:chemistry / Q000235:genetics / Q000502:physiology; D020845:Selective Estrogen Receptor Modulators / Q000494:pharmacology*
D004967:Estrogens; D008024:Ligands; D010937:Plant Growth Regulators; D011960:Receptors, Estrogen; D020845:Selective Estrogen Receptor Modulators