| Literature DB >> 28085281 |
Séverine Ravez1, Cyril Corbet2, Quentin Spillier1,2, Alice Dutu1, Anita D Robin3, Edouard Mullarky3, Lewis C Cantley3, Olivier Feron2, Raphaël Frédérick1.
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.Entities:
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Year: 2017 PMID： 28085281 PMCID： PMC5603230 DOI： 10.1021/acs.jmedchem.6b01166
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446