Androgen Receptor
The androgen receptor (AR.; NR3C4) is a type of nuclear receptor that is activated by binding either of the androgenic hormones, testosterone, or dihydrotestosterone in the cytoplasm and then translocating into the nucleus. The androgen receptor is most closely related to the progesterone receptor, and progestins in higher dosages can block the androgen receptor.
The main function of the androgen receptor is as a DNA-binding transcription factor that regulates gene expression; however, the androgen receptor has other functions as well. Androgen regulated genes are critical for the development and maintenance of the male sexual phenotype.The regulation of this integrity by androgen receptor (AR) signaling can be attributed to both osteoblasts and osteocytes.
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Andarine (S-4)是选择性雄激素受体调节剂（SARM），还是部分激动剂。
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Spironolactone是雄激素受体拮抗剂, IC50为77 nM.
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Epiandrosterone是一种类固醇激素, 具有弱雄激素活性。
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Galeterone是一种选择性CYP17抑制剂，也是androgen receptor (AR)（雄激素受体）拮抗剂，IC50分别为300 nM和384 nM，也有效抑制人类前列腺肿瘤生长。
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Ostarine是选择性雄激素受体调节剂，ED50为0.44 mg/day。
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