Anticancer efficacy of the metabolic blocker 3-bromopyruvate: specific molecular targeting.

摘要: The anticancer efficacy of the pyruvate analog 3-bromopyruvate has been demonstrated in multiple tumor models. chief principle underlying antitumor effects is its ability to effectively target energy metabolism cancer cells. Biochemically, glycolytic enzyme glyceraldehyde-3-phosphate dehydrogenase (GAPDH) identified as primary 3-bromopyruvate. Its inhibition results depletion intracellular ATP, causing cell death. Several reports have also that addition GAPDH inhibition, induction cellular stress contributes treatment-dependent apoptosis. Furthermore, recent evidence shows taken up selectively by cells via monocarboxylate transporters (MCTs) are frequently overexpressed (for export lactate produced during aerobic glycolysis). preferential uptake MCTs facilitates selective targeting while leaving healthy and non-malignant tissue untouched. Taken together, specificity molecular cells, underscore potential a potent promising agent. In this review, we highlight mechanistic characteristics discuss for translation into clinic.