中国药理学通报
中國藥理學通報
중국약이학통보
CHINESE PHARMACOLOGICAL BULLETIN
2010年
3期
289-293
,共5页
PLK1%有丝分裂%DNA%p53%肿瘤%免疫%治疗靶点
PLK1%有絲分裂%DNA%p53%腫瘤%免疫%治療靶點
PLK1%유사분렬%DNA%p53%종류%면역%치료파점
PLK1%mitosis%DNA%p53%tumor%immunity%target
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激酶1(PLK1)是高度保守的絲/囌氨痠激酶,在多種人類腫瘤細胞中高錶達.其在有絲分裂進程中的重要作用已經被闡明.最新的研究髮現, PLK1有誘導DNA閤成、DNA完整性的檢脩以及防止細胞凋亡方麵的作用.PLK1還能通過燐痠化p53而抑製其轉活性,進而抑製p53髮揮檢驗點蛋白和誘導細胞凋亡的功能.另外,PLK1與腫瘤的髮生髮展密切相關,還可以通過抑製MAVS調節榦擾素IFN的誘導生成,破壞先天性免疫.多種PLK1的抑製劑都錶現齣瞭高效低毒的特性, PLK1有望成為噁性腫瘤治療和免疫治療的良好靶點.
Polo-Like격매1(PLK1)시고도보수적사/소안산격매,재다충인류종류세포중고표체.기재유사분렬진정중적중요작용이경피천명.최신적연구발현, PLK1유유도DNA합성、DNA완정성적검수이급방지세포조망방면적작용.PLK1환능통과린산화p53이억제기전활성,진이억제p53발휘검험점단백화유도세포조망적공능.령외,PLK1여종류적발생발전밀절상관,환가이통과억제MAVS조절간우소IFN적유도생성,파배선천성면역.다충PLK1적억제제도표현출료고효저독적특성, PLK1유망성위악성종류치료화면역치료적량호파점.
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.