抑制 RRM2 以增强化疗的抗癌活性。
Inhibiting RRM2 to enhance the anticancer activity of chemotherapy.
机构信息
State Key Laboratory for Diagnosis and Treatment of Infectious Disease, National Clinical Research Center for Infectious Diseases, Collaborative Innovation Center for Diagnosis and Treatment of Infectious Diseases, Zhejiang Provincial Key Laboratory for Drug Clinical Research and Evaluation, The First Affiliated Hospital, College of Medicine, Zhejiang University, 79 QingChun Road, Hangzhou, Zhejiang 310000, People's Republic of China.
The Department of Rehabilitation Medicine, The First Affiliated Hospital, College of Medicine, Zhejiang University, 79 QingChun Road, Hangzhou, Zhejiang, 310000, People's Republic of China.
出版信息
Biomed Pharmacother. 2021 Jan;133:110996. doi: 10.1016/j.biopha.2020.110996. Epub 2020 Nov 20.
RRM2, the small subunit of ribonucleotide reductase, is identified as a tumor promotor and therapeutic target. It is common to see the overexpression of RRM2 in chemo-resistant cancer cells and patients. RRM2 mediates the resistance of many chemotherapeutic drugs and could become the predictor for chemosensitivity and prognosis. Therefore, inhibition of RRM2 may be an effective means to enhance the anticancer activity of chemotherapy. This review tries to discuss the mechanisms of RRM2 overexpression and the role of RRM2 in resistance to chemotherapy. Additionally, we compile the studies on small interfering RNA targets RRM2, RRM2 inhibitors, kinase inhibitors, and other ways that could overcome the resistance of chemotherapy or exert synergistic anticancer activity with chemotherapy through the expression inhibition or the enzyme inactivation of RRM2.
RRM2 是核糖核苷酸还原酶的小亚基，被鉴定为肿瘤促进剂和治疗靶点。在耐药性癌细胞和患者中，RRM2 的过度表达是很常见的。RRM2 介导了许多化疗药物的耐药性，可能成为化疗敏感性和预后的预测因子。因此，抑制 RRM2 可能是增强化疗抗癌活性的有效手段。本文试图探讨 RRM2 过度表达的机制以及 RRM2 在化疗耐药中的作用。此外，我们还对靶向 RRM2 的小干扰 RNA、RRM2 抑制剂、激酶抑制剂以及其他通过抑制 RRM2 的表达或酶失活来克服化疗耐药性或与化疗发挥协同抗癌活性的方法进行了综述。
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