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ID: ALA3992533
Journal: J Med Chem
Title: α-Ketothioamide Derivatives: A Promising Tool to Interrogate Phosphoglycerate Dehydrogenase (PHGDH).
Authors: Ravez S, Corbet C, Spillier Q, Dutu A, Robin AD, Mullarky E, Cantley LC, Feron O, Frédérick R.
Abstract: Given the putative role of PHGDH in cancer, development of inhibitors is required to explore its function. In this context, we established and validated a straightforward enzymatic assay suitable for high-throughput screening and we identified inhibitors with similar chemical scaffolds. Through a convergent pharmacophore approach, we synthesized α-ketothioamides that exhibit interesting in vitro PHGDH inhibition and encouraging cellular results. These novel probes may be used to understand the emerging biology of this metabolic target.
CiteXplore: 28085281