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A novel small-molecule inhibitor of 3-phosphoglycerate dehydrogenase

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Article: e1164280 | Received 07 Mar 2016, Accepted 07 Mar 2016, Published online: 31 May 2016

References

  • Snell K. Enzymes of serine metabolism in normal, developing and neoplastic rat tissues. Adv Enzyme Regul 1984; 22:325-400; PMID:6089514; http://dx.doi.org/10.1016/0065-2571(84)90021-9
  • Eagle H. Amino acid metabolism in mammalian cell cultures. Science 1959; 130(3373):432-7; http://dx.doi.org/10.1007/978-4-431-55651-0
  • Mullarky E, Mattaini KR, Vander Heiden MG, Cantley LC, Locasale JW. PHGDH amplification and altered glucose metabolism in human melanoma. Pigment Cell Melanoma Res 2011; 24:1112-5; PMID:21981974; http://dx.doi.org/10.1111/j.1755-148X.2011.00919.x
  • DeNicola GM, Chen PH, Mullarky E, Sudderth JA, Hu Z, Wu D, Tang H, Xie Y, Asara JM, Huffman KE, et al. NRF2 regulates serine biosynthesis in non-small cell lung cancer. Nat Genet 2015; 47:1475-81; PMID:26482881; http://dx.doi.org/10.1038/ng.3421
  • Locasale JW, Grassian AR, Melman T, Lyssiotis CA, Mattaini KR, Bass AJ, Heffron G, Metallo CM, Muranen T, Sharfi H, et al. Phosphoglycerate dehydrogenase diverts glycolytic flux and contributes to oncogenesis. Nat Genet 2011; 43:869-74; PMID:21804546; http://dx.doi.org/10.1038/ng.890
  • Possemato R, Marks KM, Shaul YD, Pacold ME, Kim D, Birsoy K, Sethumadhavan S, Woo HK, Jang HG, Jha AK, et al. Functional genomics reveal that the serine synthesis pathway is essential in breast cancer. Nature 2011; 476:346-50; PMID:21760589; http://dx.doi.org/10.1038/nature10350
  • Mullarky E, Lucki NC, Beheshti Zavareh R, Anglin JL, Gomes AP, Nicolay BN, Wong JCY, Christen S, Takahashi H, Singh PK, et al. Identification of a small molecule inhibitor of 3-phosphoglycerate dehydrogenase to target serine biosynthesis in cancers. Proc Natl Acad Sci USA 2016; 113:1778-83; PMID:26831078; http://dx.doi.org/10.1073/pnas.1521548113
  • Maddocks ODK, Labuschagne CF, Adams PD, Vousden KH. Serine Metabolism Supports the Methionine Cycle and DNA/RNA Methylation through De Novo ATP Synthesis in Cancer Cells. Molecular Cell 2016; 61:210-21; PMID:26774282; http://dx.doi.org/10.1016/j.molcel.2015.12.014
  • Fan J, Ye J, Kamphorst JJ, Shlomi T, Thompson CB, Rabinowitz JD. Quantitative flux analysis reveals folate-dependent NADPH production. Nature 2014; 510:298-302; PMID:24805240; http://dx.doi.org/10.1038/nature13236
  • Mullarky E, Cantley LC. Diverting Glycolysis to Combat Oxidative Stress. Innovative Med 2015; 113(7):1778–1783