4.6 Article

Inhibition of the Alanine-Serine-Cysteine-1 Transporter by BMS-466442

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

  1. Vlaams Agentschap Innoveren & Ondernemen Project [155028]

向作者/读者索取更多资源

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。

评论

主要评分

4.6
评分不足

次要评分

新颖性
-
重要性
-
科学严谨性
-
评价这篇论文

推荐

暂无数据
暂无数据