The making of a potent L-lactate transport inhibitor

The L-lactate-specific transporter SfMCT is a model SLC16 family homologue for the determination of inhibitors and potential drugs. Here, starting from a weakly-binding non-transported ligand, nanomolar affinity inhibitors of SfMCT are developed and crystal structures of the transporter-ligand compl...

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Autores principales: Patrick D. Bosshart, David Kalbermatter, Sara Bonetti, Dimitrios Fotiadis
Formato: article
Lenguaje:EN
Publicado: Nature Portfolio 2021
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Acceso en línea:https://doaj.org/article/97e83b41fe4545f685b939f7980553da
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Sumario:The L-lactate-specific transporter SfMCT is a model SLC16 family homologue for the determination of inhibitors and potential drugs. Here, starting from a weakly-binding non-transported ligand, nanomolar affinity inhibitors of SfMCT are developed and crystal structures of the transporter-ligand complexes are presented unveiling interactions at the atomic level.