[Selective estrogen receptor modulators: mechanisms of action and their tissue selectivity].
The SERMs (Selective Estrogen Receptor Modulators) exert selective agonistic or antagonistic effects on various estrogen target tissues. Conformational change of SERM-bound Estrogen Receptor (ER) and tissue specific expression patterns of transcription co-factors have been well investigated as the underlying factors of tissue selectivity of the SERMs. Nongenomic action, modulation of protein levels of ER and co-factors, and activation of other nuclear receptors, have been also reported as mechanisms of tissue selectivity by SERMs.
Azuma
Kotaro
K
Department of Geriatric Medicine, Graduate School of Medicine, University of Tokyo.
Inoue
Satoshi
S
D000818:Animals; D004967:Estrogens / Q000235:genetics / Q000502:physiology; D006801:Humans; D056892:Mediator Complex; D009687:Nuclear Proteins / Q000502:physiology; D009928:Organ Specificity / Q000235:genetics*; D011487:Protein Conformation; D011960:Receptors, Estrogen / Q000737:chemistry / Q000187:drug effects* / Q000235:genetics / Q000502:physiology; D020218:Response Elements; D020845:Selective Estrogen Receptor Modulators / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D015534:Trans-Activators / Q000502:physiology*; D014157:Transcription Factors / Q000502:physiology*; D014158:Transcription, Genetic / Q000235:genetics
C113182:DRIP, VDR interacting protein complex; D004967:Estrogens; D056892:Mediator Complex; D009687:Nuclear Proteins; D011960:Receptors, Estrogen; D020845:Selective Estrogen Receptor Modulators; D015534:Trans-Activators; D014157:Transcription Factors