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FR054 is an inhibitor of the HBP enzyme PGM3, with a remarkable anti-breast cancer effect[1].

FR054 (0.5-1 mM, 24-48 h) induces an early proliferation arrest followed by a marked cell death increase in breast cancer cells and induces apoptosis. The effect of FR054 occurs through PGM3 inhibition instead of other off-target effects[1].FR054 (250 μM, 24 h) treatment efficiently affects both N- and O-glycosylation levels in MDA-MB-231 cells[1].FR054 induces endoplasmic reticulum (ER) stress and a ROS-dependent apoptotic cell death[1].

FR054 (1000 mg/kg, ip) suppresses cancer growth in MDA-MB-231 xenograft mice[1].

[1]. Francesca Ricciardiello, et al. Inhibition of the Hexosamine Biosynthetic Pathway by targeting PGM3 causes breast cancer growth arrest and apoptosis. Cell Death Dis. 2018 Mar 7;9(3):377.

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