Article

Mechanism and Structure-Guided Optimization of SLC1A1/EAAT3-Selective Inhibitors in Kidney Cancer

2025-07-07

Abstract excerpt

Renal Cell Carcinomas (RCCs) depend metabolically on the trimeric sodium-coupled aspartate and glutamate transporter, SLC1A1/EAAT3; however, pharmacologically targeting SLC1A1 is challenging. We determined a cryo-EM structure of human SLC1A1 bound to compound 3e , a recently described SLC1A1-selective bicyclic imidazo[1,211α]pyridine-3-amine (BIA) inhibitor. 3e binds a membrane-embedded allosteric pocket accessi...

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Identifiers and source

Literature Corpus work: 6593c555-42f4-5fe7-9932-c887a9ca86a2
DOI: 10.1101/2025.07.03.663021

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