α-Ketothioamide derivatives: a promising tool to interrogate the phosphoglycerate dehydrogenase (PHGDH).
(2017) Journal of Medicinal Chemistry — (2017)
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- 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 use to understand the emerging biology of this metabolic target.
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Ravez, S., Corbet, C., Spillier, Q., Dutu, A., Robin, A. D., Mullarky, E., Cantley, L. C., Feron, O., & Frédérick, R. (2017). α-Ketothioamide derivatives: a promising tool to interrogate the phosphoglycerate dehydrogenase (PHGDH). Journal of Medicinal Chemistry. Accepted/in-press. https://doi.org/10.1021/acs.jmedchem.6b01166 (Original work published 2017)