李坤, 徐元波, 张伟, 马培志. PIM激酶及其小分子抑制剂的研究进展J. 药学学报, 2019,54(11): 1926-1939. doi: 10.16438/j.0513-4870.2019-0466
引用本文: 李坤, 徐元波, 张伟, 马培志. PIM激酶及其小分子抑制剂的研究进展J. 药学学报, 2019,54(11): 1926-1939. doi: 10.16438/j.0513-4870.2019-0466
LI Kun, XU Yuan-bo, ZHANG Wei, MA Pei-zhi. Recent advances of PIM kinase and its small-molecule inhibitorsJ. Acta Pharmaceutica Sinica, 2019,54(11): 1926-1939. doi: 10.16438/j.0513-4870.2019-0466
Citation: LI Kun, XU Yuan-bo, ZHANG Wei, MA Pei-zhi. Recent advances of PIM kinase and its small-molecule inhibitorsJ. Acta Pharmaceutica Sinica, 2019,54(11): 1926-1939. doi: 10.16438/j.0513-4870.2019-0466

PIM激酶及其小分子抑制剂的研究进展

Recent advances of PIM kinase and its small-molecule inhibitors

  • 摘要: 莫洛尼小鼠白血病病毒前病毒整合激酶(PIM)是一种结构独特的丝氨酸/苏氨酸激酶,在多种恶性血液病以及一些实体瘤中高度表达,且其表达量与癌症恶性程度和患者不良预后有关。PIM激酶通过对其底物蛋白进行磷酸化调节细胞的增殖和分化,是潜在的癌症治疗药物的作用靶标。国内外的研究机构通过文献报道了大量高活性的PIM激酶抑制剂,本文按照研究机构分类对其研究进展进行综述。

     

    Abstract: Provirus Integration in Maloney murine leukemia virus (PIM) represents a novel class of unique Ser/Thr kinase, which has been identified to be over-expressed in multiple hematological malignancies and some solid tumors, and the expression quantity correlates with malignant grade and poor prognosis in patients with cancer. PIM kinase plays important roles in regulation of cell proliferation and differentiation through the phosphorylation of its protein substrates, and it has become the emerging target for cancer treatment. A large number of highly active PIM kinase inhibitors have been reported by domestic and foreign research institutions, and the research progress will be summarized according to affiliations in this review.

     

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