?-Ketothioamide Derivatives: A Promising Tool to Interrogate Phosphoglycerate Dehydrogenase (PHGDH).
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ABSTRACT:
SUBMITTER: Ravez S
PROVIDER: S-EPMC5603230 | biostudies-literature | 2017 Feb
REPOSITORIES: biostudies-literature
Publications
α-Ketothioamide Derivatives: A Promising Tool to Interrogate Phosphoglycerate Dehydrogenase (PHGDH).
Ravez Séverine S Corbet Cyril C Spillier Quentin Q Dutu Alice A Robin Anita D AD Mullarky Edouard E Cantley Lewis C LC Feron Olivier O Frédérick Raphaël R
Journal of medicinal chemistry 20170127 4
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 e ...[more]
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