Identification of a small molecule inhibitor of 3-phosphoglycerate dehydrogenase to target serine biosynthesis in cancers.

@article{Mullarky2016IdentificationOA,
  title={Identification of a small molecule inhibitor of 3-phosphoglycerate dehydrogenase to target serine biosynthesis in cancers.},
  author={Edouard Mullarky and Natasha C Lucki and Reza Beheshti Zavareh and Justin L. Anglin and Ana P Gomes and Brandon N. Nicolay and Jenny C Y Wong and Stefan Christen and Hidenori Takahashi and Pradeep K. Singh and John Blenis and J David Warren and Sarah-Maria Fendt and John M. Asara and Gina M DeNicola and Costas A Lyssiotis and Luke L. Lairson and Lewis C. Cantley},
  journal={Proceedings of the National Academy of Sciences of the United States of America},
  year={2016},
  volume={113 7},
  pages={1778-83}
}
Cancer cells reprogram their metabolism to promote growth and proliferation. The genetic evidence pointing to the importance of the amino acid serine in tumorigenesis is striking. The gene encoding the enzyme 3-phosphoglycerate dehydrogenase (PHGDH), which catalyzes the first committed step of serine biosynthesis, is overexpressed in tumors and cancer cell lines via focal amplification and nuclear factor erythroid-2-related factor 2 (NRF2)-mediated up-regulation. PHGDH-overexpressing cells are… CONTINUE READING