Discovery of Allosteric Inhibition of Human ATP-Citrate Lyase

被引：6
|
作者：
Granchi, Carlotta [1 ]
机构：
[1] Univ Pisa, Dept Pharm, Via Bonanno 6, I-56126 Pisa, Italy
来源：
TRENDS IN PHARMACOLOGICAL SCIENCES | 2019年 / 40卷 / 06期
关键词：
D O I：
10.1016/j.tips.2019.04.008
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
ATP-citrate lyase (ACLY) is an enzyme that links glycolysis to lipid metabolism. To date only partial X-ray structures of ACLY have been solved, thus limiting the design of novel inhibitors. Wei and colleagues (published online in Nature April 3, 2019) now report the full structure of human ACLY in complex with NDI-091143, revealing an appealing allosteric inhibition mechanism for this compound.
引用
收藏
页码：364 / 366
页数：4
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