Toxoplasma histone acetylation remodelers as novel drug targets.
Toxoplasma histone acetylation remodelers as novel drug targets.
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DOI：
10.1586/eri.12.100
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发表时间：
2012-10
影响因子：
5.7
通讯作者：
Angel SO
中科院分区：
文献类型：
--
作者：
Vanagas L;Jeffers V;Bogado SS;Dalmasso MC;Sullivan WJ Jr;Angel SO
弓形虫是神经出生缺陷的主要原因，也是一种严重的机会病原体。作者和其他人发现弓形虫使用独特的核小体组成与其他因素一起支持精细的基因调控。组蛋白的翻译后修饰有助于建立全局染色质环境并协调 DNA 相关的生物过程。组蛋白乙酰化是影响基因表达的最重要的翻译后修饰之一。组蛋白乙酰转移酶和组蛋白脱乙酰酶作为潜在的药物靶点已得到深入研究。特别是，组蛋白脱乙酰酶抑制剂具有对抗顶复门寄生虫的活性，强调了它们作为一类新型抗寄生虫化合物的潜力。在这篇综述中，我们总结了关于弓形虫组蛋白乙酰转移酶和组蛋白脱乙酰酶的已知信息，并讨论了迄今为止研究的抑制剂。最后，作者讨论了一种独特的可能性，即弓形虫独特的核小体成分（含有非保守的 H2Bv 变异组蛋白）可能成为针对这种寄生虫的新型疗法的目标。
Toxoplasma gondii is a leading cause of neurological birth defects and a serious opportunistic pathogen. The authors and others have found that Toxoplasma uses a unique nucleosome composition supporting a fine gene regulation together with other factors. Post-translational modifications in histones facilitate the establishment of a global chromatin environment and orchestrate DNA-related biological processes. Histone acetylation is one of the most prominent post-translational modifications influencing gene expression. Histone acetyltransferases and histone deacetylases have been intensively studied as potential drug targets. In particular, histone deacetylase inhibitors have activity against apicomplexan parasites, underscoring their potential as a new class of antiparasitic compounds. In this review, we summarize what is known about Toxoplasma histone acetyltransferases and histone deacetylases, and discuss the inhibitors studied to date. Finally, the authors discuss the distinct possibility that the unique nucleosome composition of Toxoplasma, which harbors a nonconserved H2Bv variant histone, might be targeted in novel therapeutics directed against this parasite.
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影响因子：
56.9
作者：
Choudhary, Chunaram;Kumar, Chanchal;Mann, Matthias
通讯作者：
Mann, Matthias
影响因子：
6.7
作者：
Chaal BK;Gupta AP;Wastuwidyaningtyas BD;Luah YH;Bozdech Z
通讯作者：
Bozdech Z
影响因子：
4
作者：
Andrews, KT;Walduck, A;Parsons, PG
通讯作者：
Parsons, PG
影响因子：
2.7
作者：
Aul, RB;Oko, RJ
通讯作者：
Oko, RJ
DOI：
10.1073/pnas.0906801106
发表时间：
2009-08-18
影响因子：
11.1
作者：
Basu, Amrita;Rose, Kristie L.;Hake, Sandra B.
通讯作者：
Hake, Sandra B.