丝/苏氨酸激酶PLK1研究进展  

Research progress on serine/threonine kinase PLK1

作　　者：董宪喆[1] 张鹏[1] 毕明刚[2] 

机构地区：[1]哈尔滨商业大学生命科学与环境科学研究中心药物研究所,黑龙江哈尔滨150076 [2]中国医学科学院药用植物研究所,北京100193

出　　处：《中国药理学通报》2010年第3期289-293,共5页Chinese Pharmacological Bulletin

基　　金：国家自然科学基金资助项目(No30873090)

摘　　要：Polo-Like激酶1(PLK1)是高度保守的丝/苏氨酸激酶,在多种人类肿瘤细胞中高表达。其在有丝分裂进程中的重要作用已经被阐明。最新的研究发现,PLK1有诱导DNA合成、DNA完整性的检修以及防止细胞凋亡方面的作用。PLK1还能通过磷酸化p53而抑制其转活性,进而抑制p53发挥检验点蛋白和诱导细胞凋亡的功能。另外,PLK1与肿瘤的发生发展密切相关,还可以通过抑制MAVS调节干扰素IFN的诱导生成,破坏先天性免疫。多种PLK1的抑制剂都表现出了高效低毒的特性,PLK1有望成为恶性肿瘤治疗和免疫治疗的良好靶点。Polo-like kinase 1（PLK1）is a serine/threonine kinase which is highly conserved,and its activity is elevated in many human tumor cell lines.Lots of reports have shown that PLK1 is critical for all stages of mitosis.The newest report finds that PLK1 is required for DNA synthesis,maintenance of DNA integrity,and prevention of cell death.PLK1 physically binds to the tumor suppressor p53 in mammalian cultured cells,and inhibits its transactivation activity as well as its function in activate checkpoint protein and its pro-apoptotic function.Also PLK1 is involved in the development of tumors,and Polo-like kinase1（PLK1）regulates IFN induction by MAVS,breakdown the innate immunity.Various of inhibitors of PLK1 show the feature of high performance and low toxicity,suggesting that PLK1 may be a feasible target for cancer therapy and immunity therapy.

关 键 词：PLK1 有丝分裂 DNA P53 肿瘤 免疫 治疗靶点 

分 类 号：R-05[医药卫生] R329.25