Biochemical Characterization of Suramin as a Selective Inhibitor for the PKA-Mediated Phosphorylation of HBV Core Protein in Vitro(Biochemistry)
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概要
- 論文の詳細を見る
The inhibitory effect of suramin on the phosphorylation of GST-HBV core fusion protein (GST-Hcore) and two GST-Hcore fusion polypeptides (Hcore157B and Hcore164B) by two α-type cAMP-dependent protein kinases (PKAIα and PKAIIα) was biochemically investigated in vitro. It was found that (i) this phosphorylation was inhibited by suramin at a low concentration (IC_<50>=approx. 10nM); (ii) a relative high dose of suramin was required to inhibit an autophosphorylation of PKAIIα (IC_<50>=approx. 0.7μM) and the PKAIIα-mediated phosphorylation of histone H2B (IC_<50>=approx. 0.4μM); (iii) the PKAIIα-mediated phosphorylation of Hcore157B was more sensitive to suramin than the phosphorylation of Hcore157B by Ca^<2+>-dependent protein kinase (PKC); and (iv) suramin had a high binding affinity for Hcore157B, but not for histone H2B in vitro. These results suggest that suramin selectively inhibits the PKA-mediated phosphorylation of HBV-CP through the direct binding in vitro of suramin to the Arg-rich C-terminal region (containing three potential phosphorylation sites for PKA) on HBV-CP.
- 公益社団法人日本薬学会の論文
- 2006-09-01
著者
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Ohtsuki Kenzo
Genetical Biochem. Kitasato Univ.
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Ohtsuki Kenzo
Genetical Biochemistry And Signal Biology Graduate School Of Medical Sciences Kitasato University
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Enomoto Masato
Genetical Biochemistry And Signal Biology Graduate School Of Medical Sciences Kitasato University
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OKABE Motohito
Genetical Biochemistry, School of Allied Health Sciences, Kitasato University
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MAEDA Haruki
Genetical Biochemistry and Signal Biology, Graduate School of Medical Sciences, Kitasato University
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KUROKI Kazuyuki
Division of Cell Biology, Cancer Research Institute, Kanazawa University
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Maeda Haruki
Genetical Biochemistry And Signal Biology Graduate School Of Medical Sciences Kitasato University
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Kuroki Kazuyuki
Division Of Cell Biology Cancer Research Institute Kanazawa University
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Okabe Motohito
Genetical Biochemistry School Of Allied Health Sciences Kitasato University
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OHTSUKI Kenzo
Genetical Biochemistry and Signal Biology, Graduate School of Medical Sciences, Kitasato University
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