Identification of a novel PHGDH covalent inhibitor by chemical proteomics and phenotypic profiling
Abstract
The first rate-limiting enzyme of the serine synthesis pathway (SSP), phosphoglycerate dehydrogenase (PHGDH), is hyperactive in multiple tumors, which leads to the activation of SSP and promotes tumorigenesis. However, only a few inhibitors of PHGDH have been discovered to date, especially the covalent inhibitors of PHGDH. Here, we identified withangulatin A (WA), a natural small molecule, as a novel covalent inhibitor of PHGDH. Affinity-based...
Paper Details
Title
Identification of a novel PHGDH covalent inhibitor by chemical proteomics and phenotypic profiling
Published Date
Jan 1, 2022
Journal
Volume
12
Issue
1
Pages
246 - 261
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History