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- W2087533537 abstract "Core histone is composed of two H2A-H2B dimers and H3-H4 tetramers. Each histone have tail domain, which regulates dynamic structure of chromatin and transcription through posttranslational modifications. Histone acetylation-deacetylation is one of such epigenetic regulations of gene expression in eukaryotes. Histone deacetylase (HDAC) catalyze deacetylation of lysine residues in N-terminal domain of core histones and regulates gene transcription and expression. Inhibition of HDAC induces transcriptionally active chromatin, causing arrest of growth, differentiation and apoptosis. HDAC inhibitors are thought to be effective for neurodegenerative disorders, cardiac hypertrophy, inflammation and cancer. Using inhibitor composed of photochromic molecules, can be changed its property reversibly according to the wavelength of irradiated light, reversible site-directed regulation is thought to be achieved without displacement of solution or chemical modification to HDAC itself. In this study, we designed and synthesized three kinds of novel photochromic HDAC inhibitor, N-(2-hydroxy-5-phenylphenyl)-4-[(E)-2-phenyldiazen-1-yl]benzamide, N-phenyl-4-[(E)-2-phenyldiazen-1-yl]benzamide, and N-[4-({4-[(E)-2-phenyldiazen-1-yl]phenyl}formamido) butyl]-2-sulfanylacetamide composed of azobenzene moiety which may bind specifically to surface region, and benzamide or thiol group, which may bind to metal ion on active center , respectively. The design of the photochromic inhibitor was based on known HDAC inhibitor, which is known to affect HDAC class 1 selectively. Azobenzene moiety is placed in hydrophobic interacting region of inhibitor, therefore, it is expected that the light-induced structural change affects its affinity for HDACs. The synthesized photochromic HDAC inhibitor showed light-induced isomerization, derived from azobenzene moiety. Both of the cis and trans isomers of the inhibitor showed inhibitory effect of human whole HDAC activity. The trans-isomer of photochromic HDAC inhibitors showed higher inhibitory effect to HDAC in hela nuclear extract than cis isomer." @default.
- W2087533537 created "2016-06-24" @default.
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- W2087533537 date "2014-01-01" @default.
- W2087533537 modified "2023-09-28" @default.
- W2087533537 title "Design and Synthesis of a Novel Photochromic HDAC Inhibitor and its Photo Reversible Inhibitory Effect" @default.
- W2087533537 doi "https://doi.org/10.1016/j.bpj.2013.11.2712" @default.
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