Chen Fengquan, Liu Chunxi, Zhang Jian, Xu Wenfang, Zhang Yingjie
Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012 Ji'nan, Shandong, China.
Department of Pharmacy, Qilu Hospital, Shandong University, 107 West Culture Road, Ji'nan 250012, China.
Anticancer Agents Med Chem. 2018;18(9):1241-1251. doi: 10.2174/1871521409666170412123500.
The Cyclin-Dependent Kinases (CDKs) and their cyclin partners are key regulators of the cell cycle. These kinases are closely related to oncogenesis and have been proved to be attractive targets for designing novel anticancer agents. The CDK inhibitors can effectively suppress the excessive proliferation of tumor cells by inducing cell cycle arrest. In recent years, a large number of CDK inhibitors have entered pre-clinical and/or clinical trials. Among these compounds, the selective CDK4/6 inhibitor Palbociclib has been approved by FDA for breast cancer treatment. Moreover, Palbociclib demonstrated promising antitumor potential as monotherapy or combined therapy in numerous clinical trials. Herein, we provide a brief review focused on the recent progress of clinical studies about Palbociclib.
细胞周期蛋白依赖性激酶（CDKs）及其细胞周期蛋白伴侣是细胞周期的关键调节因子。这些激酶与肿瘤发生密切相关，已被证明是设计新型抗癌药物的有吸引力的靶点。CDK抑制剂可通过诱导细胞周期停滞有效抑制肿瘤细胞的过度增殖。近年来，大量CDK抑制剂已进入临床前和/或临床试验。在这些化合物中，选择性CDK4/6抑制剂哌柏西利已获美国食品药品监督管理局（FDA）批准用于乳腺癌治疗。此外，哌柏西利在众多临床试验中作为单药治疗或联合治疗均显示出有前景的抗肿瘤潜力。在此，我们简要综述了关于哌柏西利临床研究的最新进展。
