期刊
TRENDS IN BIOCHEMICAL SCIENCES
卷 32, 期 7, 页码 342-349出版社
ELSEVIER SCIENCE LONDON
DOI: 10.1016/j.tibs.2007.05.005
关键词
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资金
- NIGMS NIH HHS [U54 GM074898] Funding Source: Medline
Cancer-specific mutations in the catalytic subunit of phosphatidylinositol 3-kinase (PI3K) p110 alpha occur in diverse tumors in frequencies that can exceed 30%. The majority of these mutations map to one of three hot spots; in the gene, and the rest are distributed over much of the PI3K coding sequence. Most of the cancer-specific mutations induce a gain of function that results in oncogenicity, elevated lipid kinase activity and constitutive signaling through the kinases Akt and TOR. The location of the mutations on a model structure of p110 alpha indicates several distinct mechanisms for the gain of function. The mutated p110 alpha proteins are promising cancer targets. Although identification of mutant-specific small-molecule inhibitors seems technically challenging, the therapeutic benefits from such inhibitors could be extremely important.
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