Antiproliferative and proapoptotic activities of 4-hydroxybenzoic acid-based inhibitors of histone deacetylases

4-羟基苯甲酸类组蛋白去乙酰化酶抑制剂的抗增殖和促凋亡活性

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作者:Carole Seidel, Michael Schnekenburger, Mario Dicato, Marc Diederich

Abstract

Histone acetyltransferases (HATs) and histone deacetylases (HDACs) regulate cellular processes by modifying the acetylation status of many proteins. Pathologically altered HDAC activity contributes to cancer development and thus characterization of novel acetylation modulators is important for future anti-cancer therapies. In this study, we identified three novel 4-hydroxybenzoic acid derivatives as pan-HDAC inhibitors that increased protein acetylation levels, arrested cell cycle progression and triggered apoptotic cell death, without affecting viability of normal cells. Our data support the potential of 4-hydroxybenzoic acid derivatives as pan-HDAC inhibitors with anticancer properties.

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