靶向抑制CDK4/6的肿瘤治疗基础研究与临床应用进展

周期蛋白依赖性激酶4/6(cyclin-dependent kinase 4/6，CDK4/6) 是一类丝氨酸/苏氨酸激酶，通过与细胞周期蛋白D（cyclin D）结合，调节视网膜母细胞瘤蛋白(Rb)的磷酸化状态，Rb磷酸化后与E2F转录因子分离，释放的E2F可以自由激活一系列基因表达，参与DNA复制和细胞分裂，从而介导细胞G1/S期转换，影响细胞周期的进程。近年研究发现CDK4/6在多种肿瘤发生和发展过程中起着核心作用，已成为临床多种肿瘤治疗的重要分子靶点。本文将对CDK4/6与肿瘤的关系以及CDK4/6抑制剂临床应用的最新研究进展做一综述。

Progress in basic research and clinical application of CDK4/6 inhibitor in tumor therapy

Cyclin-dependent kinase 4/6 (CDK4/6) is a serine/threonine kinase that regulates the phosphorylation state of retinoblastoma protein (Rb) by binding to cyclin D.Phosphorylated Rb releases E2F that freely activates a series of gene expression to participate in DNA replication and cell division, which mediates cell G1/S phase transition, affects the progression of the cell cycle. Recent studies have found that CDK4/6 plays a central role in tumorigenesis and development, and has become an important molecular target for clinical treatment of various tumors. This article will review the latest research progress in the relationship between CDK4/6 and tumors and the clinical application of CDK4/6 inhibitors.