蛋白激酶2抑制剂克服表皮生长因子受体-酪氨酸激酶抑制剂耐药的有效机制

表皮生长因子受体-酪氨酸激酶抑制剂（EGFR-TKIs）在肺癌治疗中发挥着重要作用，同时EGFR-TKIs的耐药也成为了肺癌治疗领域的一大难题。近年来的研究表明，蛋白激酶2（CK2）的表达及激活失衡在肿瘤的发生、发展中发挥重要作用，且CK2抑制剂已被多次证实具有抗肿瘤疗效。文章中阐述了EGFR-TKIs的抗肿瘤作用机制以及可能的耐药机制，结合CK2的作用机制及目前CK2抑制剂在抗肿瘤治疗领域的表现，发现了EGFR与CK2下游信号通路存在交联，抑制CK2将有可能克服EGFR-TKI耐药现象。...

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Bibliographic Details
Published in中华肿瘤杂志 Vol. 38; no. 5; pp. 321 - 324
Main Author 周瑜 张盛 李珂 董晓荣 刘莉 伍钢 孟睿
Format Journal Article
LanguageChinese
Published 华中科技大学同济医学院附属协和医院肿瘤中心, 武汉,430023%华中科技大学同济医学院药剂科, 武汉,430023 2016
Subjects
抗药性
肺肿瘤
肿瘤
蛋白激酶2
表皮生长因子受体-酪氨酸激酶抑制剂
Drug resistance,neoplasm
蛋白激酶2
表皮生长因子受体-酪氨酸激酶抑制剂
抗药性,肿瘤
Protein kinase 2
肺肿瘤
Subject words] Lung neoplasms
Epidermal growth factor receptor-tyrosine kinase inhibitors
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Summary:表皮生长因子受体-酪氨酸激酶抑制剂（EGFR-TKIs）在肺癌治疗中发挥着重要作用，同时EGFR-TKIs的耐药也成为了肺癌治疗领域的一大难题。近年来的研究表明，蛋白激酶2（CK2）的表达及激活失衡在肿瘤的发生、发展中发挥重要作用，且CK2抑制剂已被多次证实具有抗肿瘤疗效。文章中阐述了EGFR-TKIs的抗肿瘤作用机制以及可能的耐药机制，结合CK2的作用机制及目前CK2抑制剂在抗肿瘤治疗领域的表现，发现了EGFR与CK2下游信号通路存在交联，抑制CK2将有可能克服EGFR-TKI耐药现象。
Bibliography:Nowadays, EGFR-TKIs are important treatment strategy in lung cancer, but the resistance to EGFR-TKIs remains an unsolved issue preventing the patients from further benefits. Recent studies have shown that casein kinase （CK2） plays an important role in carcinogenesis and development of cancer. CK2 inhibitor has also demonstrated anti-tumor effects. Here we reviewed the mechanism of EGFR- TKIs and the potential reasons of resistance. Interestingly, there is a crosstalk between CK2 and EGFR downstream signaling pathways, therefore, it may be possible that CK2 inhibitor can overcome the EGFR- TKIs resistance.
11-2152/R
Zhou Yu, Zhang Sheng, Li Ke, Dong Xiaorong, Liu Li, Wu Gang, Meng Rui（ Cancer Center, Union Hospital, Tongfi Medical College, Huazhong University of Science and Technology, Wuhan 430023, China, Department of Pharmacy, Union Hospital, Tongii Medical College, Huazhong University of Science and Technology, Wuhan 430023, China）
Lung neoplasms; Epidermal growth factor receptor-tyrosine kinase inhibitors;Pr
ISSN:0253-3766
DOI:10.3760/cma.j.issn.0253-3766.2016.05.001