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From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2022-04-29 , DOI: 10.1021/acs.jmedchem.1c02064
Zhenfeng Shi 1 , Lei Tian 2, 3 , Taotao Qiang 2 , Jingyi Li 3 , Yue Xing 3 , Xiaodong Ren 4 , Chang Liu 5 , Chengyuan Liang 3
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2022-04-29 , DOI: 10.1021/acs.jmedchem.1c02064
Zhenfeng Shi 1 , Lei Tian 2, 3 , Taotao Qiang 2 , Jingyi Li 3 , Yue Xing 3 , Xiaodong Ren 4 , Chang Liu 5 , Chengyuan Liang 3
Affiliation
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Herein, we discuss more than 50 cyclin-dependent kinase (CDK) inhibitors that have been approved or have undergone clinical trials and their therapeutic application in multiple cancers. This review discusses the design strategies, structure–activity relationships, and efficacy performances of these selective or nonselective CDK inhibitors. The theoretical basis of early broad-spectrum CDK inhibitors is similar to the scope of chemotherapy, but because their toxicity is greater than the benefit, there is no clinical therapeutic window. The notion that selective CDK inhibitors have a safer therapeutic potential than pan-CDK inhibitors has been widely recognized during the research process. Four CDK4/6 inhibitors have been approved for the treatment of breast cancer or for prophylactic administration during chemotherapy to protect bone marrow and immune system function. Furthermore, the emerging strategies in the field of CDK inhibitors are summarized briefly, and CDKs continue to be widely pursued as emerging anticancer drug targets for drug discovery.
中文翻译：
从结构修饰到药物上市：对用于多种癌症治疗的细胞周期蛋白依赖性激酶抑制剂的持续发展的系统评价
在此，我们讨论了超过 50 种已获批准或已进行临床试验的细胞周期蛋白依赖性激酶 (CDK) 抑制剂及其在多种癌症中的治疗应用。本综述讨论了这些选择性或非选择性 CDK 抑制剂的设计策略、构效关系和功效表现。早期广谱CDK抑制剂的理论基础与化疗的范围相似，但由于其毒性大于益处，因此不存在临床治疗窗口。在研究过程中，选择性 CDK 抑制剂比泛 CDK 抑制剂具有更安全的治疗潜力这一概念已得到广泛认可。四种 CDK4/6 抑制剂已被批准用于治疗乳腺癌或在化疗期间预防性给药，以保护骨髓和免疫系统功能。此外，简要总结了 CDK 抑制剂领域的新兴策略，CDK 作为药物发现的新兴抗癌药物靶点继续被广泛追捧。
更新日期：2022-04-29
中文翻译：
从结构修饰到药物上市：对用于多种癌症治疗的细胞周期蛋白依赖性激酶抑制剂的持续发展的系统评价
在此，我们讨论了超过 50 种已获批准或已进行临床试验的细胞周期蛋白依赖性激酶 (CDK) 抑制剂及其在多种癌症中的治疗应用。本综述讨论了这些选择性或非选择性 CDK 抑制剂的设计策略、构效关系和功效表现。早期广谱CDK抑制剂的理论基础与化疗的范围相似，但由于其毒性大于益处，因此不存在临床治疗窗口。在研究过程中，选择性 CDK 抑制剂比泛 CDK 抑制剂具有更安全的治疗潜力这一概念已得到广泛认可。四种 CDK4/6 抑制剂已被批准用于治疗乳腺癌或在化疗期间预防性给药，以保护骨髓和免疫系统功能。此外，简要总结了 CDK 抑制剂领域的新兴策略，CDK 作为药物发现的新兴抗癌药物靶点继续被广泛追捧。
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