Identification of a new membrane-permeable inhibitor against inositol-1,4,5-trisphosphate-3-kinase A.

Biochemical and Biophysical Research Communications(2013)

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摘要
•Identification of an inhibitor (BAMB-4) of the InsP3kinases activity of the metastasis-promoting protein ITPKA.•BAMB-4 is completely absorbed by lung tumor cells without showing any degradation after cellular uptake.•BAMB-4 is relative specific and does not belong to the group of typical kinase inhibitors.•BAMB-4 is a mixed type inhibitor affecting both substrates of InsP3kinase, InsP3 and ATP, which increases its specificity.•BAMB-4 for the first time provides the possibility to effectively inhibit InsP3kinase-activity in tumor cells.
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关键词
Metastasis,High-throughput screening,ITPKA,InsP3,Cellular uptake,Mixed inhibition type,ITPKA-inhibitor
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