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Negative allosteric modulator of 3-phosphoglycerate dehydrogenase (PHGDH)
Negative allosteric modulator of phosphoglycerate dehydrogenase (PHGDH) (IC50 = 34.8 μM). Exhibits antitumor activity in vitro in breast cancer cells lines overexpressing PHGDH (EC50 values are 7.7 and 10.8 μM in MDA-MB-468 and HCC-70 cells, respectively). Inhibits growth of MDA-MB-468 xenografts in mice.
Wang et al (2017) Rational design of selective allosteric inhibitors of PHGDH and serine synthesis with anti-tumor activity. Cell Chem.Biol. 24 55 PMID:28042046
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