期刊
ACS CHEMICAL NEUROSCIENCE
卷 10, 期 5, 页码 2510-2517出版社
AMER CHEMICAL SOC
DOI: 10.1021/acschemneuro.9b00019
关键词
asc1; transporter; mutagenesis; binding mode; homology model; SDM; SLC7A10
资金
- Vlaams Agentschap Innoveren & Ondernemen Project [155028]
Experiment and modeling were combined to understand inhibition of the alanine-serine-cysteine-1 (asc1) transporter. The structure-activity relationship (SAR) was explored with synthesis of analogues of BMS-466442. Direct target interaction and binding site location between TM helices 6 and 10 were confirmed via site directed mutagenesis. Computational modeling suggested the inhibitor binds via competitive occupation of the orthosteric site while also blocking the movement of TM helices that are required for transport.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据