| Budget Amount *help |
¥5,460,000 (Direct Cost: ¥4,200,000、Indirect Cost: ¥1,260,000)
Fiscal Year 2013: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2012: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2011: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
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| Research Abstract |
Bendamustine (Benda) is an anti-lymphoma drug, which was recently approved in Japan. Although DNA has been believed to be primary target of this agent, the details of mechanism of action still remain unclear. We herein, for the first time, report STAT3 inhibition by Benda. The STAT3-SH2 antagonistic activity was shown by Benda but not by the inactive metabolites in the biochemical assay using recombinant human STAT3 protein. Furthermore, Benda suppressed both DNA-binding and transcriptional activity of STAT3 in the human breast cancer cell line MDA-MB-463. The competitive pull-down assay using the Benda analogs revealed that this agent tightly bound to cellular STAT3. Therefore, those results suggest that the previously reported anti-cancer and immunomodulation effects by this agent might be associated with its inhibitory effect on STAT3.
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