摘要
蛋白激酶是细胞功能的关键调节分子,参与编排绝大多数细胞活动,组成了纵横交错的调节网络。调节细胞蛋白活性中起关键作用的激酶是抗癌药物的主要靶标,因为它们的异常形式可以促进肿瘤细胞的增殖。Polo样激酶-1(Plk-1)是丝氨酸/苏氨酸(Ser/Thr)激酶polo样家族成员之一,参与调节细胞增殖的有丝分裂过程的多个方面,是真核细胞有丝分裂的关键激酶之一,它的过表达与人类许多癌症的发生发展密切相关。针对Plk-1的药物开发可能是治疗癌症的前景方向之一。本文将总结Plk-1的结构特征和参与的细胞过程,以及针对Plk-1抗肿瘤治疗的基本原理和抑制剂开发的最新进展和最新策略。
Protein kinases are key regulators of cellular function and constitute one of the largest and participate in orch estrating the vast majority of cellular activities,forming a criss-cross regulatong network.Kinases,which play a key role in regulating the activity of cellular proteins,are prime targets for anticancer drugs because their abnormal forms can promote the proliferation of tumor cells.Polo-like kinase-1(Plk-1)is a member of the polo-like family of serine/threonine(Ser/Thr)kinases,which is involved in many aspects of the mitotic process that regulates cell proliferation,which is one of the key kinases of cell mitosis,whose overexpression is closely related to the occurrence and development of many human cancers.Drug development targeting Plk-1 may be one of the promising directions for the treatment of cancer.This review will summarize the structural features of Plk-1 and the cellular processes involved,as well as the rationale for anti-tumor therapy against Plk-1,the latest progress in inhibitor development and the latest strategies.
作者
潘冰
贺强
Pan Bing;He Qiang(Department of Hepatobiliary Surgery,Beijing Chaoyang Hospital,Capital Medical University,Beijing 100020,China)
出处
《国际外科学杂志》
2022年第9期644-648,共5页
International Journal of Surgery
基金
北京市自然科学基金(7212042)。