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α-Ketothioamide Derivatives: A Promising Tool to Interrogate Phosphoglycerate Dehydrogenase (PHGDH).

Date Posted: February 8, 2017

Titleα-Ketothioamide Derivatives: A Promising Tool to Interrogate Phosphoglycerate Dehydrogenase (PHGDH).
Publication TypeJournal Article
Year of Publication2017
AuthorsRavez S, Corbet C, Spillier Q, Dutu A, Robin AD, Mullarky E, Cantley LC, Feron O, Frédérick R
JournalJ Med Chem
Date Published2017 Jan 27
ISSN1520-4804
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.

DOI10.1021/acs.jmedchem.6b01166
Alternate JournalJ. Med. Chem.
PubMed ID28085281