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细胞周期蛋白依赖性激酶(CDKs)活性的精确调控对细胞的增殖和转录至关重要,对于一些增殖性疾病特别是恶性肿瘤,细胞的生长和增殖失控与CDKs活性异常密切相关。对CDK2蛋白结构的认识,特别是一些抑制剂与CDK2复合物的晶体学认识,极大的推动了小分子抑制剂的设计和开发。本文对一些骨架相异的有临床开发价值的小分子抑制剂与CDK2激酶的相互作用进行了解析,对激酶的各结合区特征做了归纳,进而分析了目前该领域的研究状况和趋势。
Precise regulation of cyclin-dependent kinase (CDKs) activity is crucial for cell proliferation and transcription. For some proliferative diseases, especially malignant tumors, the uncontrolled growth and proliferation of cells and CDKs activity are closely related. The understanding of CDK2 protein structure, especially the crystallographic understanding of some inhibitors and CDK2 complex, greatly promoted the design and development of small molecule inhibitors. In this paper, we analyzed the interactions between CDK2 kinase and some small molecule inhibitors with different skeletons, and summarized the characteristics of each binding region of kinases, and then analyzed the current research status and trends in this field.