二甲基姜黄素（ASC-J9）对雄激素受体相关疾病作用及分子机制的研究进展。
A review of the effects and molecular mechanisms of dimethylcurcumin (ASC-J9) on androgen receptor-related diseases.
机构信息
National & Local Joint Engineering Research Center for High-efficiency Refining and High-quality Utilization of Biomass, School of Pharmaceutical Engineering and Life Sciences, Changzhou University, Changzhou, China.
Center for Health Science and Engineering, School of Materials Science and Engineering, Hebei University of Technology, Tianjin, China.
出版信息
Chem Biol Drug Des. 2021 Apr;97(4):821-835. doi: 10.1111/cbdd.13811. Epub 2021 Jan 11.
Dimethylcurcumin (ASC-J9) is a curcumin analogue capable of inhibiting prostate cancer cell proliferation. The mechanism is associated with the unique role of ASC-J9 in enhancing androgen receptor (AR) degradation. So far, ASC-J9 has been investigated in typical AR-associated diseases such as prostate cancer, benign prostatic hypertrophy, bladder cancer, renal diseases, liver diseases, cardiovascular diseases, cutaneous wound, spinal and bulbar muscular atrophy, ovarian cancer and melanoma, exhibiting great potentials in disease control. In this review, the effects and molecular mechanisms of ASC-J9 on various AR-associated diseases are summarized. Importantly, the effects of ASC-J9 and AR antagonists enzalutamide/bicalutamide on prostate cancer are compared in detail and crucial differences are highlighted. At last, the pharmacological effects of ASC-J9 are summarized and the future applications of ASC-J9 in AR-associated disease control are discussed.
二甲基姜黄素（ASC-J9）是一种姜黄素类似物，能够抑制前列腺癌细胞增殖。其作用机制与 ASC-J9 独特的增强雄激素受体（AR）降解的作用有关。迄今为止，ASC-J9 已在典型的 AR 相关疾病中进行了研究，如前列腺癌、良性前列腺增生、膀胱癌、肾脏疾病、肝脏疾病、心血管疾病、皮肤创伤、脊髓和延髓性肌肉萎缩、卵巢癌和黑色素瘤，在疾病控制方面显示出巨大的潜力。在这篇综述中，总结了 ASC-J9 对各种 AR 相关疾病的作用和分子机制。重要的是，详细比较了 ASC-J9 和 AR 拮抗剂恩扎鲁胺/比卡鲁胺对前列腺癌的作用，并强调了关键差异。最后，总结了 ASC-J9 的药理学作用，并讨论了 ASC-J9 在 AR 相关疾病控制中的未来应用。
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