| Budget Amount *help |
¥5,200,000 (Direct Cost: ¥4,000,000、Indirect Cost: ¥1,200,000)
Fiscal Year 2016: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2015: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2014: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
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| Outline of Final Research Achievements |
We previously discovered a novel STAT3 inhibitor, STX-COMP, which is expected to be a new anticancer drug candidate. The investigation on the mode of action of STX-COMP and identification of its susceptibility factors are important issues for the purpose of clinical use of this unique compound in future. In this study, we demonstrated STX-COMP inhibits STAT3 dimerization and thereby suppress the transcriptional activity in cancer cells. The profile of this compound in the various bioassays was proved to be quite different from other known STAT3 inhibitors. Furthermore, we revealed that STX-COMP not only inhibited the growth of cancer cells but also suppressed the expression of immune checkpoint factors such as PD-L1 and IDO1 in cancer cells. To identify the biomarker for STX-COMP, we refined the susceptibility factor candidates to the STAT3 inhibition by using the siRNA library. The kinase inhibitors that might be useful for the combination therapies with STX-COMP were also discovered.
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