Identification of new p300 histone acetyltransferase inhibitors from natural products by a customized virtual screening method

被引：24

作者：

Li, Guo-Bo ^{[1
]}

Huang, Lu-Yi ^{[1
]}

Li, Hui ^{[1
]}

Ji, Sen ^{[1
]}

Li, Lin-Li ^{[2
]}

Yang, Sheng-Yong ^{[1
]}

机构：

[1] Sichuan Univ, West China Hosp, State Key Lab Biotherapy, West China Med Sch,Collaborat Innovat Ctr Biother, Chengdu 610041, Sichuan, Peoples R China

[2] Sichuan Univ, West China Sch Pharm, Key Lab Drug Targeting & Drug Delivery Syst, Minist Educ, Chengdu 610041, Sichuan, Peoples R China

来源：

RSC ADVANCES | 2016年 / 6卷 / 66期

基金：

中国国家自然科学基金;

关键词：

SCORING FUNCTION; ACETYLATION;

D O I：

10.1039/c6ra11240d

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Herein, we sought to discover new p300 HAT inhibitors from natural products by a customized structure-based virtual screening method. The natural compounds NP-2 (spinosine), NP-3 (palmatine), NP-9 (venenatine), and NP-15 (taxodione) were found to be potent p300 HAT inhibitors, of which IC50 values are 0.69 mu M, 1.05 mu M, 0.58 mu M, 4.85 mu M, respectively.

引用

页码：61137 / 61140

页数：4

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