Macrocyclic histone deacetylase inhibitors.
Macrocyclic histone deacetylase inhibitors.
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DOI：
10.2174/156802610792232079
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发表时间：
2010
影响因子：
3.4
通讯作者：
Oyelere AK
中科院分区：
文献类型：
--
作者：
Mwakwari SC;Patil V;Guerrant W;Oyelere AK
组蛋白去乙酰化酶抑制剂（HDACi）是一类新兴的新型抗癌药物，可引起肿瘤细胞的生长抑制、分化和凋亡。此外，它们还显示出抗寄生虫，抗神经退行性疾病，抗风湿病和免疫抑制剂的前景。迄今为止，已经报道了几种结构独特的小分子HDACi，包括芳基羟酸酯、苯酰胺、短链脂肪酸、亲电酮和大环肽。大环HDACi具有最复杂的帽基，与HDAC酶的外环相互作用，具有良好的HDAC抑制效力和异构体选择性。本文就大环HDACi的研究进展及现状作一综述。
Histone deacetylase inhibitors (HDACi) are an emerging class of novel anti-cancer drugs that cause growth arrest, differentiation, and apoptosis of tumor cells. In addition, they have shown promise as anti-parasitic, anti-neurodegenerative, anti-rheumatologic and immunosuppressant agents. To date, several structurally distinct small molecule HDACi have been reported including aryl hydroxamates, benzamides, short-chain fatty acids, electrophilic ketones, and macrocyclic peptides. Macrocyclic HDACi possess the most complex cap-groups which interact with HDAC enzyme’s outer rim and have demonstrated excellent HDAC inhibition potency and isoform selectivity. This review focuses on the recent progress and current state of macrocyclic HDACi.