大环组蛋白去乙酰化酶抑制剂。
Macrocyclic histone deacetylase inhibitors.
机构信息
Parker H. Petit Institute of Bioengineering and Bioscience, Georgia Institute of Technology, Atlanta, 30332-0400, USA.
出版信息
Curr Top Med Chem. 2010;10(14):1423-40. doi: 10.2174/156802610792232079.
Abstract
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.
摘要
组蛋白去乙酰化酶抑制剂（HDACi）是一类新兴的抗癌药物，能使肿瘤细胞生长停滞、分化并凋亡。此外，它们还表现出抗寄生虫、抗神经退行性疾病、抗风湿和免疫抑制的作用。迄今为止，已经报道了几种结构不同的小分子 HDACi，包括芳基羟肟酸、苯甲酰胺、短链脂肪酸、亲电酮和大环肽。大环 HDACi 具有最复杂的盖帽基团，与 HDAC 酶的外边缘相互作用，并表现出优异的 HDAC 抑制活性和同工酶选择性。本综述重点介绍了大环 HDACi 的最新进展和现状。
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