Experimental Therapeutics Programme, Spanish National Cancer Research Centre, Madrid, Spain.
Instituto de Biomedicina de Sevilla (IBiS), HUVR/CSIC/Universidad de Sevilla, Sevilla, Spain; Consejo Superior de Investigaciones Cientificas, Spain.
Biochem Pharmacol. 2013 Mar 1;85(5):629-643. doi: 10.1016/j.bcp.2012.09.018. Epub 2012 Oct 5.
PIM proteins belong to a family of ser/thr kinases composed of 3 members, PIM1, PIM2 and PIM3, with greatly overlapping functions. PIM kinases are mainly responsible for cell cycle regulation, antiapoptotic activity and the homing and migration of receptor tyrosine kinases mediated via the JAK/STAT pathway. PIM kinases have been found to be upregulated in many hematological malignancies and solid tumors. Although these kinases have been described as weak oncogenes, they are heavily targeted for anticancer drug discovery. The present review summarizes the discoveries made to date regarding PIM kinases as driving oncogenes in the process of tumorigenesis and their validation as drug targets.
PIM 蛋白属于丝氨酸/苏氨酸激酶家族，由 3 个成员组成，即 PIM1、PIM2 和 PIM3，它们具有高度重叠的功能。PIM 激酶主要负责细胞周期调控、抗凋亡活性以及通过 JAK/STAT 通路介导的受体酪氨酸激酶的归巢和迁移。已经发现 PIM 激酶在许多血液恶性肿瘤和实体瘤中上调。尽管这些激酶被描述为弱癌基因，但它们是抗癌药物发现的重要靶点。本综述总结了迄今为止关于 PIM 激酶作为致癌基因在肿瘤发生过程中的发现及其作为药物靶点的验证。
