Since its discovery almost a century ago (Warburg), the times-fold increase in glycolysis in cancer has been a well-studied impact in cancer research for many years, if not decades, and it is now recognised as the most significant characteristic of cancer. As a result, some researchers have recently suggested that inhibiting glycolysis in cancer cells might be a promising cancer therapy. Among the glycolysis inhibitors tested, 3-bromopyruvate, a pyruvate analogue, piqued the interest of researchers in the area, probably because it was thought to be particularly selective for cancer cells immediately after the first tests. In order to improve the therapeutic efficacy of this approach, it is tentatively suggested in this study that derivatives of 3-bromopyruvate, glucose or deoxyglucose, some marked with the positron emitting 18F or the beta minus emitting 83Br, and a non-radioactive glucose with a Br atom on the C6 could be used as anticancer agents. After finding a well-differentiated uptake between cancer and normal tissues (ratio of uptake/kg in cancer to the same in the whole body greater than 10) and replacing 18F with the radioactive 83Br in the pyruvate molecule in an attempt to introduce a radioactive isotope emitting beta minus radiation, the researchers tried substituting 18F with the radioactive 83Br in the pyruvate molecule.
Dipartimento di Scienze Biomediche Sperimentali, Via Colombo 3 Padova, Italy.
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