Pooneh Koochaki on Muck Rack

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

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By Biao Qiu, Jesse A. Coker, Pooneh Koochaki
| biorxiv.org
Abstract 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[1,2-α]pyridine-3-amine (BIA) inhibitor.
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