Characterization of Alkylbenzene Sulfonate Inhibitors of Protein Phosphatase 1α Activity

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  • アルキルベンゼンスルホン酸によるプロテインホスファターゼ1α活性への阻害作用の研究
  • アルキルベンゼンスルホンサン ニ ヨル プロテインホスファターゼ 1aカッセイ エ ノ ソガイ サヨウ ノ ケンキュウ
  • Characterization of Alkylbenzene Sulfonate Inhibitors of Protein Phosphatase 1α Activity

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Abstract

Background & Aims: Protein phosphatase 1 (PP1) is a member of the phosphoprotein phosphatase (PPP) family which, together with protein phosphatase 2A and protein phosphatase 2B (PP2B), exhibits serine/threonine phosphatase activity. We previously reported that linear alkylbenzenesulfonates (LAS) noncompetitively inhibit the phosphatase activity of calcineurin (CN), also known as PP2B. Here we examined the inhibitory effect of LAS on PP1α activity and determined the mechanism of inhibition.<br>Methods: The inhibitory effect of LAS against PP1α enzymatic activity was confirmed using p -nitrophenylphosphate as a substrate and was further examined by kinetic analysis.<br>Results: C12-LAS to C14-LAS exhibited strong inhibitory effects for PP1α. The half maximal inhibitory concentration (IC50) value of C12-LAS was 13.2μM. Using a double-reciprocal plot, C12-LAS was determined to exhibit uncompetitive inhibitory effects on PP1α activity.<br>Conclusions: LAS analogues containing twelve to fourteen carbons in the alkyl side chain showed strong inhibitory effects against both PP1α and CN. Although LAS shows noncompetitive inhibition for CN, our results demonstrate that it exhibits uncompetitive inhibition for PP1α.

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