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Redirecting raltitrexed from cancer cell thymidylate synthase to Mycobacterium tuberculosis phosphopantetheinyl transferase

15 Mar 2024

Abstract excerpt

There is a compelling need to find drugs active against Mycobacterium tuberculosis ( Mtb ). 4′-Phosphopantetheinyl transferase (PptT) is an essential enzyme in Mtb that has attracted interest as a potential drug target. We optimized a PptT assay, used it to screen 422,740 compounds, and identified raltitrexed, an antineoplastic antimetabolite, as the most potent PptT inhibitor yet reported. While trying...

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PMID: 38489355
DOI: 10.1126/sciadv.adj6406

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