PIM1激酶的分子结构及其在肿瘤中的表达调控研究进展  

Research Progress on the Molecular Structure of PIM1 Kinase and Its Expression Regulation in Tumors

作　　者：许茜茜 毛雨婷 朱欣 XU Qianqian;MAO Yuting;ZHU Xin(Postgraduate Training Base Alliance of Wenzhou Medical University,Zhejiang Cancer Hospital,Hangzhou 310022,China;Key Laboratory of Head&Neck Cancer Translational Research of Zhejiang Province,Zhejiang Cancer Hospital,Hangzhou 310022,China)

机构地区：[1]温州医科大学研究生培养基地,浙江省肿瘤医院,浙江杭州310022 [2]浙江省头颈肿瘤转化医学研究重点实验室,浙江省肿瘤医院,浙江杭州310022

出　　处：《肿瘤学杂志》2024年第10期859-865,共7页Journal of Chinese Oncology

基　　金：国家自然科学基金(82072950)。

摘　　要：PIM1激酶作为具有丝氨酸和(或)苏氨酸激酶活性的原癌基因莫罗尼小鼠白血病病毒前病毒整合位点(PIM)家族成员,与肿瘤的发生及进展息息相关,是肿瘤治疗的重要靶点。PIM1激酶主要调节三大类行为,包括肿瘤发生、保护细胞免受凋亡信号和逃避免疫攻击。全文总结PIM1激酶的分子结构,阐述PIM1激酶ATP结合口袋及其组成性活性;从转录、翻译、翻译后修饰水平对其表达调控进行阐述,归纳了对应调控因子。以分子结构和转录调控作为切入点,展望了PIM1抑制剂的治疗现状,并对PIM1抑制剂提出了新的观点与启发。As a member of the proviral insertion in murine malignancies family of proto-oncogenes expressing serine and/or threonine kinase activity, PIM1 kinase is closely related to the occurrence and development of tumors and is an important target for tumor treatment. PIM1 kinases primarily deal with three broad categories of functions such as tumorigenesis, protecting cells from apoptotic signals and evading immune attacks. This paper detailed the constitutive activity and ATP-binding pocket of PIM1 kinase in addition to summarizing the enzyme's molecular structure. Its expression was regulated at the transcription, translation, and post-translational stages;the associated regulatory factors were also enumerated. Taking molecular structure and transcriptional regulation as the starting point, this paper looks forward to the treatment status of PIM1 inhibitors, and puts forward new perspectives and enlightenment for PIM1 inhibitors.

关 键 词：PIM1 肿瘤 靶向治疗 表达调控 

分 类 号：R730[医药卫生—肿瘤]