期刊
FUTURE ONCOLOGY
卷 6, 期 9, 页码 1461-1478出版社
FUTURE MEDICINE LTD
DOI: 10.2217/FON.10.106
关键词
antiapoptotic; biomarker cell cycle arrest; DNA repair drug target; genomic instability; PIM1 serine/threonine kinase; SGI-1776
类别
资金
- NIH [RO1 GM071760, RO1 CA104470]
- NATIONAL CANCER INSTITUTE [R01CA104470] Funding Source: NIH RePORTER
- NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES [R01GM071760] Funding Source: NIH RePORTER
The highly conserved proto-oncogenic protein PIM1 is an unusual serine or threonine kinase, in part because it is constitutively active. Overexpression of PIM1 experimentally leads to tumor formation in mice, while complete knockout of the protein has no observable phenotype. It appears to contribute to cancer development in three major ways when it is overexpressed: by inhibiting apoptosis, by promoting cell proliferation and by promoting genomic instability. Expression in normal tissues is nearly undetectable. However, in hematopoietic malignancies and in a variety of solid tumors, increased PIM1 expression has been shown to correlate with the stage of disease. This characteristic suggests it can serve as a useful biomarker for cancer diagnosis and prognosis. Several specific and potent inhibitors of PIM1 's kinase activity have also been shown to induce apoptotic death of cancer cells, to sensitize cancer cells to chemotherapy and to synergize with other anti-tumor agents, thus making it an attractive therapeutic target.
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