α-Ketothioamide Derivatives: A Promising Tool to Interrogate Phosphoglycerate Dehydrogenase (PHGDH) Academic Article uri icon

Overview

MeSH Major

  • Enzyme Inhibitors
  • Phosphoglycerate Dehydrogenase
  • Thioamides

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.

publication date

  • February 23, 2017

Research

keywords

  • Academic Article

Identity

Language

  • eng

PubMed Central ID

  • PMC5603230

Digital Object Identifier (DOI)

  • 10.1021/acs.jmedchem.6b01166

PubMed ID

  • 28085281

Additional Document Info

start page

  • 1591

end page

  • 1597

volume

  • 60

number

  • 4