Journal
ACS CHEMICAL NEUROSCIENCE
Volume 10, Issue 5, Pages 2510-2517Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acschemneuro.9b00019
Keywords
asc1; transporter; mutagenesis; binding mode; homology model; SDM; SLC7A10
Funding
- Vlaams Agentschap Innoveren & Ondernemen Project [155028]
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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.
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