靶向泛素-蛋白酶体系统用于癌症治疗的小分子
The Small Molecules Targeting Ubiquitin-Proteasome System for Cancer Therapy.
作者信息
Ao Nannan, Chen Qianping, Liu Geng
机构信息
School of Radiation Medicine and Protection, Medical College of Soochow University, Collaborative Innovation Center of Radiological Medicine of Jiangsu Higher Education Institutions, Suzhou 215123. China.
出版信息
Comb Chem High Throughput Screen. 2017;20(5):403-413. doi: 10.2174/1386207320666170710124746.
BACKGROUND & AIM: The ubiquitin-proteasome system (UPS) is the major pathway for degrading the intracellular proteins. The 2004 Nobel Prize in Chemistry was awarded to Rose, Hershko, and Ciechanover to highlight the fundamental importance of UPS.
METHOD & RESULTS: The alterations in this process have been shown to contribute to the cancer progression. Hence, UPS has become a popular target for developing chemotherapeutics against tumours. The application of bortezomib showed high efficiency in treating haematological malignancies by interfering with UPS activity. Many compounds are being screened and evaluated in recent pharmacological advances, either as single agents or in synergy with other drugs, and more to be revealed.
CONCLUSION
In the present review, we exhibit the crucial ingredients involved in UPS and discuss the current situation of small molecules targeting various components of ubiquitination pathway in cancer treatment.
背景与目的
泛素-蛋白酶体系统（UPS）是细胞内蛋白质降解的主要途径。2004年诺贝尔化学奖授予了罗斯、赫什科和切哈诺沃，以彰显UPS的根本重要性。
方法与结果
该过程的改变已被证明与癌症进展有关。因此，UPS已成为开发抗肿瘤化疗药物的热门靶点。硼替佐米的应用通过干扰UPS活性在治疗血液系统恶性肿瘤方面显示出高效性。在最近的药理学进展中，许多化合物正在作为单一药物或与其他药物协同作用进行筛选和评估，还有更多有待揭示。
结论
在本综述中，我们展示了UPS中涉及的关键成分，并讨论了在癌症治疗中靶向泛素化途径各个组分的小分子的现状。
Zotero 插件