3-BrOP is a cell-permeable ester of the the glycolysis inhibitor 3-bromopyruvate (3-BrPA) that is known to target hexokinase II (HK2) and GAPDH. Upon entering the cells, 3-BrOP is hydrolyzed by intracellular esterase to 3-BrPA. 3-BrOP is shown to synergize cancer cell killing with mTOR inhibitor rapamycin (apoptosis induction with/without 100 ng/mL rapamycin = 64%/36% of Raji human lymphoma cells by 40 μM 3-BrOP and 72%/45% of HL-60 leukemia cells by 20 μM 3-BrOP in 24 h) due to enhanced cellular ATP depletion and glucose uptake inhibition. When administered via tail vein injection, 3-BrOP significantly suppersses SK-N-SH xenograft-derived neuroblastoma tumor growth in mice in vivo (by 78% in 14 days; 20 mg/kg/day).
Cell-permeable ester of the the glycolysis inhibitor 3-bromopyruvate (3-BrPA) with in vitro and in vivo anti-cancer efficacy.
Investigational new drugs, 30(1), 191-199 (2010-10-05)
Children with high-risk and recurrent neuroblastoma have poor survival rates, and novel therapies are needed. Many cancer cells have been found to preferentially employ the glycolytic pathway for energy generation, even in the presence of oxygen. 3-BrOP is a novel
The mammalian target of rapamycin (mTOR) pathway plays important roles in regulating nutrient metabolism and promoting the growth and survival of cancer cells, which exhibit increased glycolysis for ATP generation. In this study, we tested the hypothesis that inhibition of
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