Effect of ZSTK474, a Novel Phosphatidylinositol 3-Kinase Inhibitor, on DNA-Dependent Protein Kinase(Pharmacology)
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概要
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Phosphatidylinositol 3-kinase (P13K) has been implicated in a variety of diseases including cancer. A number of P13K inhibitors have recently been developed for use in cancer therapy. ZSTK474 is a highly promising antitumor agent targeting P13K. We previously reported that ZSTK474 showed potent inhibition against four class I P13K isoforms but not against 140 protein kinases. However, whether ZSTK474 inhibits DNA-dependent protein kinase (DNA-PK), which is structurally similar to P13K, remains unknown. To investigate the inhibition of DNA-PK, we developed a new DNA-PK assay method using Kinase-Glo. The inhibition activity of ZSTK474 against DNA-PK was determined, and shown to be far weaker compared with that observed against P13K. The inhibition selectivity of ZSTK474 for P13K over DNA-PK was significantly higher than other P13K inhibitors, namely NVP-BEZ235, PI-103 and LY294002. These results indicated that ZSTK474 was the most specific agent among these P13K inhibitors.
- 公益社団法人日本薬学会の論文
- 2009-02-01
著者
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Yamori Takao
Division Of Experimental Chemotherapy Cancer Chemotherapy Center Japanese Foundation For Cancer
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Kong Dexin
Division Of Molecular Pharmacology Cancer Chemotherapy Center Japanese Foundation For Cancer Researc
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Yamori Takao
Division Of Molecular Pharmacology Cancer Chemotherapy Center Japanese Foundation For Cancer Researc
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Yaguchi Shin-ichi
Division Of Molecular Pharmacology Cancer Chemotherapy Center Japanese Foundation For Cancer Researc
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Kong Dexin
Division Of Molecular Pharmacology Cancer Chemotherapy Center Japanese Foundation For Cancer Researc
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