Inhibiting PHGDH with NCT-503 reroutes glucose-derived carbons into the TCA cycle, independently of its on-target effect

Inhibiting PHGDH with NCT-503 reroutes glucose-derived carbons into the TCA cycle, independently of its on-target effect

The small-molecule inhibitor of phosphoglycerate dehydrogenase, NCT-503, reduces incorporation of glucose-derived carbons into serine in vitro. Here we describe an off-target effect of NCT-503 in neuroblastoma cell lines expressing divergent phosphoglycerate dehydrogenase (PHGDH) levels and single-c...

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Bibliographic Details
Main Authors: Birte Arlt, Guido Mastrobuoni, Jasmin Wuenschel, Kathy Astrahantseff, Angelika Eggert, Stefan Kempa, Hedwig E. Deubzer
Format: Article
Language:English
Published: Taylor & Francis Group 2021-01-01
Series:Journal of Enzyme Inhibition and Medicinal Chemistry
Subjects:
cancer cell metabolism
de novo serine synthesis pathway
citrate synthase
pulsed stable isotope-resolved metabolomics
thermal shift assay
Online Access:http://dx.doi.org/10.1080/14756366.2021.1935917

Internet

http://dx.doi.org/10.1080/14756366.2021.1935917

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