谢宝花, 胡志烨, 宁文涛, 杨录, 周海兵. 针对乳腺癌治疗的PROTACs研究进展J. 药学学报, 2020,55(9): 2053-2061. doi: 10.16438/j.0513-4870.2020-0340
引用本文: 谢宝花, 胡志烨, 宁文涛, 杨录, 周海兵. 针对乳腺癌治疗的PROTACs研究进展J. 药学学报, 2020,55(9): 2053-2061. doi: 10.16438/j.0513-4870.2020-0340
XIE Bao-hua, HU Zhi-ye, NING Wen-tao, YANG Lu, ZHOU Hai-bing. The research progress of PROTACs for breast cancer treatmentJ. Acta Pharmaceutica Sinica, 2020,55(9): 2053-2061. doi: 10.16438/j.0513-4870.2020-0340
Citation: XIE Bao-hua, HU Zhi-ye, NING Wen-tao, YANG Lu, ZHOU Hai-bing. The research progress of PROTACs for breast cancer treatmentJ. Acta Pharmaceutica Sinica, 2020,55(9): 2053-2061. doi: 10.16438/j.0513-4870.2020-0340

针对乳腺癌治疗的PROTACs研究进展

The research progress of PROTACs for breast cancer treatment

  • 摘要: 乳腺癌是全球女性发病率最高的恶性肿瘤。在乳腺癌肿瘤组织中,观察到多种与乳腺癌发生和发展相关的靶标,针对这些靶标,已有不少药物在临床上应用。然而这些药物大多数属于小分子抑制剂,随着药物的长期使用,不少患者体内会产生耐药性。因此,克服耐药性问题以及开发更加有效的药物成为目前乳腺癌治疗中急需解决的问题。蛋白水解靶向嵌合体(proteolysis targeting chimera,PROTAC)技术是一种新型的靶向蛋白降解技术,在药物研发领域已经表现出良好的应用前景。运用PROTAC技术靶向降解乳腺癌中的相关靶点,有望成为乳腺癌治疗中切实可行的策略之一。

     

    Abstract: Breast cancer is the most common malignant tumor in women worldwide. In breast cancer tumor tissues, a variety of targets related to the occurrence and development of breast cancer have been observed, and many drugs have been used in clinical applications for these targets. However, most of these drugs are small molecule inhibitors. With the long-term use of these drugs, acquired drug resistance often occurs in breast cancer patients. To overcome the drug resistance, the development of more efficient drugs is highly desirable in the treatment of breast cancer. Proteolysis targeting chimera (PROTAC) technology is a new kind of targeted protein degradation technology, which has shown broad prospect of applications in the field of drug development. The use of PROTAC technology to target the degradation of relevant targets in breast cancer has become a feasible strategy for breast cancer treatment.

     

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