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The Search for Potent, Small‐Molecule HDACIs in Cancer Treatment: A Decade After Vorinostat
Medicinal Research Reviews ( IF 13.3 ) Pub Date : 2017-02-09 , DOI: 10.1002/med.21437
Chiara Zagni 1 , Giuseppe Floresta 1, 2 , Giulia Monciino 1 , Antonio Rescifina 1
Affiliation  

Histone deacetylases (HDACs) play a crucial role in the remodeling of chromatin, and are involved in the epigenetic regulation of gene expression. In the last decade, inhibition of HDACs came out as a target for specific epigenetic changes associated with cancer and other diseases. Until now, more than 20 HDAC inhibitors (HDACIs) have entered clinical studies, and some of them (e.g., vorinostat, romidepsin) have been approved for the treatment of cutaneous T‐cell lymphoma. This review provides an overview of current knowledge, progress, and molecular mechanisms of HDACIs, covering a period from 2011 until 2015.

中文翻译:

寻找有效的小分子HDACI用于癌症治疗:伏立诺他后的十年

组蛋白脱乙酰基酶(HDAC)在染色质的重塑中起关键作用,并参与基因表达的表观遗传调控。在过去的十年中,HDAC的抑制作用成为与癌症和其他疾病相关的特定表观遗传学改变的目标。迄今为止,已有20多种HDAC抑制剂(HDACI)进入临床研究,其中一些(例如伏立诺他,罗米地辛)已被批准用于治疗皮肤T细胞淋巴瘤。这篇综述概述了HDACI的当前知识,进展和分子机制,涵盖了从2011年到2015年的时间。
更新日期:2017-02-09
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