PHGDH

PHGDH

The NAD+-dependent enzyme 3-phosphoglycerate dehydrogenase (PHGDH; EC 1.1.1.95), which catalyzes the first committed step of serine biosynthesis from glucose via the phosphoserine pathway, is overexpressed in tumors and cancer cell lines via focal amplification and nuclear factor erythroid-2-related factor 2 (NRF2)-mediated up-regulation. Since it was found that proliferation of PHGDH-amplified cancer cell lines, and other lines that overexpress PHGDH without amplification, is inhibited by PHGDH knockdown, PHGDH inhibitors as a targeted therapy for these tumor types represent an exciting clinical opportunity.

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  • CBR 5884
    2585
    CBR 5884
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    2623
    NCT-503
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More About PHGDH

The NAD+-dependent enzyme 3-phosphoglycerate dehydrogenase (PHGDH; EC 1.1.1.95), which catalyzes the first committed step of serine biosynthesis from glucose via the phosphoserine pathway, is overexpressed in tumors and cancer cell lines via focal amplification and nuclear factor erythroid-2-related factor 2 (NRF2)-mediated up-regulation. Since it was found that proliferation of PHGDH-amplified cancer cell lines, and other lines that overexpress PHGDH without amplification, is inhibited by PHGDH knockdown, PHGDH inhibitors as a targeted therapy for these tumor types represent an exciting clinical opportunity[1].

[1] E Mullarky et al. Identification of a small molecule inhibitor of 3-phosphoglycerate dehydrogenase to target serine biosynthesis in cancers. Proc Natl Acad Sci U S A. 2016 Feb 16;113(7):1778-83.

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