共 69 条
Zinc binding groups for histone deacetylase inhibitors
被引:183
作者:

Zhang, Lei
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机构:
Weifang Med Univ, Sch Pharm, Dept Med Chem, Weifang, Shandong, Peoples R China Weifang Med Univ, Sch Pharm, Dept Med Chem, Weifang, Shandong, Peoples R China

Zhang, Jian
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Weifang Med Univ, Sch Pharm, Dept Med Chem, Weifang, Shandong, Peoples R China Weifang Med Univ, Sch Pharm, Dept Med Chem, Weifang, Shandong, Peoples R China

Jiang, Qixiao
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机构:
Qingdao Univ, Sch Pharm, Qingdao, Shandong, Peoples R China Weifang Med Univ, Sch Pharm, Dept Med Chem, Weifang, Shandong, Peoples R China

Zhang, Li
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h-index: 0
机构:
Qingdao Univ, Sch Pharm, Qingdao, Shandong, Peoples R China Weifang Med Univ, Sch Pharm, Dept Med Chem, Weifang, Shandong, Peoples R China

Song, Weiguo
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h-index: 0
机构:
Weifang Med Univ, Sch Pharm, Dept Med Chem, Weifang, Shandong, Peoples R China Weifang Med Univ, Sch Pharm, Dept Med Chem, Weifang, Shandong, Peoples R China
机构:
[1] Weifang Med Univ, Sch Pharm, Dept Med Chem, Weifang, Shandong, Peoples R China
[2] Qingdao Univ, Sch Pharm, Qingdao, Shandong, Peoples R China
关键词:
Histone deacetylase inhibitor;
zinc binding group;
anti-tumour;
selectivity;
drug design;
PHASE-I;
CARDIAC-HYPERTROPHY;
VALPROIC ACID;
ORAL CI-994;
POTENT;
COMBINATION;
IDENTIFICATION;
MGCD0103;
CANCER;
ST7612AA1;
D O I:
10.1080/14756366.2017.1417274
中图分类号:
Q5 [生物化学];
Q7 [分子生物学];
学科分类号:
071010 ;
081704 ;
摘要:
Zinc binding groups (ZBGs) play a crucial role in targeting histone deacetylase inhibitors (HDACIs) to the active site of histone deacetylases (HDACs), thus determining the potency of HDACIs. Due to the high affinity to the zinc ion, hydroxamic acid is the most commonly used ZBG in the structure of HDACs. An alternative ZBG is benzamide group, which features excellent inhibitory selectivity for class I HDACs. Various ZBGs have been designed and tested to improve the activity and selectivity of HDACIs, and to overcome the pharmacokinetic limitations of current HDACIs. Herein, different kinds of ZBGs are reviewed and their features have been discussed for further design of HDACIs.
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收藏
页码:714 / 721
页数:8
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