喵ID：K6hRWn
A 'click' chemistry approach to novel entinostat (MS-275) based class I histone deacetylase proteolysis targeting chimeras. A 'click' chemistry approach to novel entinostat (MS-275) based class I histone deacetylase proteolysis targeting chimeras.
A 'click' chemistry approach to novel entinostat (MS-275) based class I histone deacetylase proteolysis targeting chimeras.
A 'click' chemistry approach to novel entinostat (MS-275) based class I histone deacetylase proteolysis targeting chimeras.基本信息
DOI：
10.1039/d2md00199c
10.1039/d2md00199c发表时间：
2022-12-14
2022-12-14影响因子：
4.1
4.1通讯作者：
中科院分区：
医学3区
医学3区文献类型：
Journal Article
Journal Article 作者：
研究方向： --
MeSH主题词： --
关键词： --
来源链接：pubmed详情页地址
文献摘要
Click chemistry was utilised to prepare a library of PROTACs based on entinostat a class I histone deacetylase (HDAC) inhibitor in clinical trials. A novel PROTAC JMC-137 was identified as a HDAC1/2 and HDAC3 degrader in HCT116 cells. However, potency was compromised compared to previously identified class I HDAC PROTACs highlighting the importance in the choice of HDAC ligand, functional group for linker attachment and positioning in PROTAC design.
Click chemistry was utilised to prepare a library of PROTACs based on entinostat a class I histone deacetylase (HDAC) inhibitor in clinical trials.
利用点击化学制备了一个基于恩替诺特（一种处于临床试验阶段的I类组蛋白去乙酰化酶（HDAC）抑制剂）的蛋白降解靶向嵌合体（PROTACs）库。一种新型的PROTAC JMC - 137在HCT116细胞中被鉴定为HDAC1/2和HDAC3降解剂。然而，与先前鉴定的I类HDAC PROTACs相比，其效力有所降低，这凸显了在PROTAC设计中选择HDAC配体、连接子连接的官能团以及定位的重要性。
利用点击化学制备了一个基于恩替诺特（一种处于临床试验阶段的I类组蛋白去乙酰化酶（HDAC）抑制剂）的蛋白降解靶向嵌合体（PROTACs）库。
参考文献（0）
被引文献（0）
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2021-12-29影响因子：
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0作者：
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