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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DHEA (Dehydroisoandrosterone)是内源性甾体激素，可作为神经类固醇，与多种核与细胞表面受体相结合。
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ARN-509是一种选择性的，竞争性的androgen receptor抑制剂，IC50为16 nM，有效治疗前列腺癌。
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Bicalutamide (比卡鲁胺; Casodex) 是口服的非甾体抗雄激素化合物，能与雄激素受体结合，可作用于前列腺癌，IC50为0.16 μM。
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Enzalutamide, an AR signaling inhibitor, is effective for bicalutamide-resistant tumors and has been used in metastatic castration-resistant prostate cancer. Enzalutamide (MDV3100)是一种雄激素受体(AR)拮抗剂，IC50为36 nM。
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