Wu Wen, Lu Cheng, Chen Si-yu, Yu Nie-fang
Institute of Molecular Design and Drug Discovery, School of Pharmaceutical Sciences, Central South University, Changsha 410013, China.
Yao Xue Xue Bao. 2009 Mar;44(3):242-57.
Signal transduction in cells plays an important role in the process of cellular metabolism, segmentation, differentiation, biological behaviors and cell death. Direct and indirect involvement of kinases in tumor growth, metastasis and apoptosis make them the most promising targets for anticancer discovery. Most of the kinase inhibitors in clinical use or in late development stages are multi-target kinase inhibitors (MTKIs). These MTKIs are demonstrated to exert potent anti-tumor effects through several different pathways. This review presents in the view of a medicinal chemistry point, a brief account and analysis of transduction pathways of representative MTKIs in clinical use or in late development stages.
细胞中的信号转导在细胞代谢、分裂、分化、生物学行为及细胞死亡过程中发挥着重要作用。激酶直接或间接参与肿瘤生长、转移及凋亡,使其成为抗癌药物研发中最具潜力的靶点。大多数临床使用或处于后期研发阶段的激酶抑制剂都是多靶点激酶抑制剂(MTKIs)。这些MTKIs已被证明可通过多种不同途径发挥强大的抗肿瘤作用。本综述从药物化学角度,简要介绍并分析了临床使用或处于后期研发阶段的代表性MTKIs的信号转导途径。