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Description: CBR-5884 is a novel, potent, and selective inhibitor of phosphoglycerate dehydrogenase (PHGDH) with an IC50 of 33 uM and with anticancer activities. CBR-5884 inhibits de novo serine synthesis in cancer cells and is selectively toxic to cancer cell lines with high serine biosynthetic activity. CBR-5884 selectively inhibits the proliferation of melanoma and breast cancer lines that have a high propensity for serine synthesis. Biochemical characterization of the inhibitor revealed that it was a noncompetitive inhibitor that showed a time-dependent onset of inhibition and disrupted the oligomerization state of PHGDH.
References: Proc Natl Acad Sci U S A, 2016 Feb 16, 113(7):1778-83.
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