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KMID : 0043320120350081379
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Archives of Pharmacal Research
2012 Volume.35 No. 8 p.1379 ~ p.1386
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Inhibition of PCAF histone acetyltransferase and cytotoxic effect of N-acylanthranilic acids
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Park Woong-Jae
Ma Eun-Sook
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Abstract
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Small molecule HAT inhibitors are useful tools to unravel the role of histone acetyltransferases (HATs) in the cell and have relevance for oncology. We synthesized a series of N-acylanthranilic acids (11?16) and of N-acyl-5-hydroxyanthranilic acids (17?22) bearing C6, C8, C10, C12, C14, along with C16 acyl chain at the 2-amino position of anthranilic acid or 5-hydroxyanthranilic acid. Enzyme inhibition of these compounds was investigated, using invitro PCAF HAT assays. All synthesized compounds (65?76%) showed similar inhibitory activity to anacardic acid (68%) at 100 μM. The cytotoxicity, against one normal cell line (HSF) and eight cancer cell lines (HT-29, HCT-116, MDA-231, A-549, Hep3B, Caski, HeLa and Caki), were evaluated by the SRB method.
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KEYWORD
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Histone acetyltransferase (HAT), p300/CBP associated factor (PCAF), Cytotoxicity, N-Acylanthranilic acid
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