A novel small-molecule inhibitor of 3-phosphoglycerate dehydrogenase

Edouard Mullarky; Luke L Lairson; Lewis C Cantley; Costas A Lyssiotis

doi:10.1080/23723556.2016.1164280

A novel small-molecule inhibitor of 3-phosphoglycerate dehydrogenase

Mol Cell Oncol. 2016 Mar 30;3(4):e1164280. doi: 10.1080/23723556.2016.1164280. eCollection 2016 Jul.

Authors

Edouard Mullarky¹, Luke L Lairson², Lewis C Cantley³, Costas A Lyssiotis⁴

Affiliations

¹ Meyer Cancer Center, Weill Cornell Medical College, New York, NY, USA; Department of Medicine, Weill Cornell Medical College, New York, NY, USA; Biological and Biomedical Sciences Graduate Program, Harvard Medical School, Boston, MA, USA.
² Department of Chemistry, The Scripps Research Institute, North Torrey Pines, La Jolla, CA, USA; The California Institute for Biomedical Research, North Torrey Pines, La Jolla, CA, USA.
³ Meyer Cancer Center, Weill Cornell Medical College, New York, NY, USA; Department of Medicine, Weill Cornell Medical College, New York, NY, USA.
⁴ Department of Molecular and Integrative Physiology, University of Michigan, Ann Arbor, MI, USA; Department of Internal Medicine, Division of Gastroenterology, University of Michigan, Ann Arbor, MI, USA.

Abstract

Serine metabolism is likely to play a critical role in cancer cell growth. A recent study reports the identification of a novel small-molecule inhibitor of serine synthesis that targets 3-phosphoglycerate dehydrogenase (PHGDH), the first enzyme of the serine synthesis pathway, and selectively abrogates the proliferation of PHGDH overexpressing breast cancer cells.

Keywords: 3-phosphoglycerate dehydrogenase; PHGDH; cancer metabolism; serine.

Abstract

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