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View article: A Yeast‐Based Assay for Inhibitors of <scp>l</scp>‐Lactate Transport Utilizing Fluorescent Biosensors
A Yeast‐Based Assay for Inhibitors of <span>l</span>‐Lactate Transport Utilizing Fluorescent Biosensors Open
Inhibitors of ʟ‐lactate transport are in development as a novel mode of action in antitumor therapy and malaria. Previously, we used radiolabeled ʟ‐lactate to assay transport via the human monocarboxylate transporter 1, MCT1, and the struc…
View article: Addressing the Intracellular Vestibule of the Plasmodial Lactate Transporter PfFNT by p-Substituted Inhibitors Amplifies In Vitro Activity
Addressing the Intracellular Vestibule of the Plasmodial Lactate Transporter PfFNT by p-Substituted Inhibitors Amplifies In Vitro Activity Open
Inhibition of the lactate transporter PfFNT is a valid novel mode of action against malaria parasites. Current pyridine-substituted pentafluoro-3-hydroxy-pent-2-en-1-ones act as substrate analogs with submicromolar EC50 in vitro, and >99.7…