使用 'Androgen Receptor' 作为标签的产品
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Androgen Receptor 激动剂
Andarine (GTX-007)是研究性的选择性雄激素受体调节剂（SARM）。
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Androgen Receptor 抑制剂
Apalutamide (ARN-509)是一种具有潜在抗肿瘤活性的雄激素受体拮抗剂，IC50 为 16 nM。ARN-509与靶组织中的AR结合，从而阻止了雄激素诱导的受体激活，并促进了无法转运至细胞核的无活性复合物的形成。这防止了AR应答基因的结合和转录。
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- Frédérique Mittler, .et al. High-Content Monitoring of Drug Effects in a 3D Spheroid Model, Front Oncol, 2017, 7: 293 PMID: 29322028
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AR 抑制剂 downregulator
AZD3514是一种有效的雄激素受体下调剂，具有潜在的抗癌活性。
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Androgen Receptor 拮抗剂
Bicalutamide (Casodex)是一种口服非甾体抗雄激素，用于治疗前列腺癌和多毛症。
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- Mi Chen, .et al. TRIM33 drives prostate tumor growth by stabilizing androgen receptor from Skp2-mediated degradation, EMBO Rep, 2022, Aug 3;23(8):e53468 PMID: 35785414
- Takashi Azuma, .et al. Removal of pharmaceuticals in water by introduction of ozonated microbubbles, SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Anowara Khatun, .et al. Transcriptional Repression and Protein Degradation of the Ca2+-Activated K+ Channel KCa1.1 by Androgen Receptor Inhibition in Human Breast Cancer Cells, Front Physiol, 2018, 9: 312 PMID: 29713287
- Azuma T, .et al. Distribution of six anticancer drugs and a variety of other pharmaceuticals, and their sorption onto sediments, in an urban Japanese river, Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. Detection of pharmaceuticals and phytochemicals together with their metabolites in hospital effluents in Japan, and their contribution to sewage treatment plant influents, Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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Androgen Receptor 拮抗剂
Cyproterone acetate是17-羟孕酮的合成衍生物，可作为雄激素受体拮抗剂以及具有弱孕激素和糖皮质激素活性的弱孕激素受体激动剂。
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Dehydroepiandrosterone是一种重要的内源性类固醇激素。
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Androgen Receptor 拮抗剂
EPI-001是雄激素受体（AR）的拮抗剂，它通过与AR的N末端结构域（NTD）共价结合并阻断AR及其剪接变体（转录因子IC50）的转录活性所需的蛋白质相互作用抑制AR NTD反式激活6μM）
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Androgen receptor 拮抗剂
Flutamide是一种抗雄激素药物，其活性代谢洛丽塔与Ki值为55nM的雄激素受体结合，可作用于前列腺癌。
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Androgen receptor 拮抗剂
MDV3100(Enzalutamide)是一种androgen-receptor (AR)拮抗剂。在AR研究中强烈推荐的抑制剂。
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- Shiv Verma, .et al. Increased cytokine gene expression and cognition risk associated with androgen deprivation therapy, Prostate, 2022, Oct;82(14):1389-1399 PMID: 35821621
- Mi Chen, .et al. TRIM33 drives prostate tumor growth by stabilizing androgen receptor from Skp2-mediated degradation, EMBO Rep, 2022, Aug 3;23(8):e53468 PMID: 35785414
- Prem P Kushwaha, .et al. Role of solute carrier transporters SLC25A17 and SLC27A6 in acquired resistance to enzalutamide in castration-resistant prostate cancer, Mol Carcinog, 2021, Dec 22 PMID: 34939235
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Megestrol Acetate是具有抗肿瘤特性的孕酮衍生物。
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Androgen receptor 拮抗剂
ODM-201是一种有效且完全的人类AR（hAR）拮抗剂，IC50值为26 nM。
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CYP17 抑制剂
TOK-001 (Galeterone)既是雄激素受体拮抗剂又是CYP17A1抑制剂。
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