Center for Transdisciplinary Research, Department of Pharmacology, Saveetha Dental College and Hospitals, Saveetha Institute of Medical and Technical Sciences (SIMATS), Saveetha University, Chennai, Tamil Nadu, India.
Adv Protein Chem Struct Biol. 2023;135:313-342. doi: 10.1016/bs.apcsb.2023.02.003. Epub 2023 Mar 8.
Cancer has been linked to the uncontrolled proliferation of cells and the overexpression of cell-cycle genes. The cell cycle machinery plays a crucial role in the regulation of the apoptosis to mitosis to growth phase progression. The mechanisms of the cell cycle also play an important role in preventing DNA damage. There are multiple members of the protein kinase family that are involved in the activities of the cell cycle. Essential cyclins effectively regulate cyclin-dependent kinases (CDKs), which are themselves adversely regulated by naturally occurring CDK inhibitors. Despite the fact that various compounds can effectively block the cell cycle kinases and being investigated for their potential to fight cancer. This chapter explains the detail of cell cycle and checkpoint regulators, that are crucial to the malignant cellular process. The known CDKs inhibitors and their mechanism of action in various cancers have also been addressed as a step toward the development of a possibly novel technique for the design of new drugs against cell cycle kinase proteins.
癌症与细胞的不受控制的增殖和细胞周期基因的过度表达有关。细胞周期机制在调节细胞凋亡、有丝分裂和生长阶段进展方面起着至关重要的作用。细胞周期的机制在防止 DNA 损伤方面也起着重要作用。蛋白激酶家族的多个成员参与细胞周期的活动。必需的细胞周期蛋白有效地调节细胞周期蛋白依赖性激酶(CDK),而 CDK 本身又受到天然存在的 CDK 抑制剂的不利调节。尽管有多种化合物可以有效地阻断细胞周期激酶,并正在研究它们在对抗癌症方面的潜力。本章详细说明了细胞周期和检查点调节剂,这对恶性细胞过程至关重要。还讨论了已知的 CDK 抑制剂及其在各种癌症中的作用机制,这是朝着开发针对细胞周期激酶蛋白的新型药物设计技术迈出的一步。