3-Bromopyruvate
Bromopyruvate (3-BrPA) is a glycolysis inhibitor that has been reported to have a strong anti-tumour effect in many human tumours. Several studies have reported that 3-BrPA could inhibit glioma progression; however, its role on the interstitial cells in the glioma microenvironment has not been investigated. In previous studies, Sheng et al. found that in the glioma microenvironment, glioma stem cells can induce the malignant transformation of macrophages and dendritic cells. In a study, they focused on the effects of 3-BrPA on malignantly transformed macrophages and dendritic cells. First, they found that 3-BrPA inhibited the proliferation of malignantly transformed macrophages and dendritic cells in a dose-dependent and time-dependent manner. Further study indicated that 3-BrPA significantly decreased extracellular lactate and inhibited the clone formation, migration and invasion of malignantly transformed macrophages and dendritic cells. Using an online database and a series of experiments, they demonstrated that 3-BrPA inhibits the malignant progression of malignantly transformed macrophages and dendritic cells via the miR-449a/MCT1 axis. These findings built experimental basis for new approach against glioma 1).
Unclassified
Chen TC, Yu J, Nouri Nigjeh E, Wang W, Myint PT, Zandi E, Hofman FM, Schönthal AH. A perillyl alcohol-conjugated analog of 3-bromopyruvate without cellular uptake dependency on monocarboxylate transporter 1 and with activity in 3-BP-resistant tumor cells. Cancer Lett. 2017 Aug 1;400:161-174. doi: 10.1016/j.canlet.2017.04.015. Epub 2017 Apr 24. PubMed PMID: 28450161.
3: Tomizawa M, Shinozaki F, Motoyoshi Y, Sugiyama T, Yamamoto S, Ishige N. Differentiation of Human-induced pluripotent stem cells in William's E initiation medium supplemented with 3‑bromopyruvate and 2‑deoxy‑d‑glucose. Mol Med Rep. 2017 Jun;15(6):3719-3723. doi: 10.3892/mmr.2017.6474. Epub 2017 Apr 12. PubMed PMID: 28440498.
4: Tran Q, Lee H, Park J, Kim SH, Park J. Targeting Cancer Metabolism - Revisiting the Warburg Effects. Toxicol Res. 2016 Jul;32(3):177-93. doi: 10.5487/TR.2016.32.3.177. Epub 2016 Jul 30. Review. PubMed PMID: 27437085; PubMed Central PMCID: PMC4946416.
5: Tomizawa M, Shinozaki F, Motoyoshi Y, Sugiyama T, Yamamoto S, Ishige N. Suppressive effects of 3-bromopyruvate on the proliferation and the motility of hepatocellular carcinoma cells. Oncol Rep. 2016 Jan;35(1):59-63. doi: 10.3892/or.2015.4370. Epub 2015 Nov 2. PubMed PMID: 26530887.
6: Wicks RT, Azadi J, Mangraviti A, Zhang I, Hwang L, Joshi A, Bow H, Hutt-Cabezas M, Martin KL, Rudek MA, Zhao M, Brem H, Tyler BM. Local delivery of cancer-cell glycolytic inhibitors in high-grade glioma. Neuro Oncol. 2015 Jan;17(1):70-80. doi: 10.1093/neuonc/nou143. Epub 2014 Jul 22. PubMed PMID: 25053853; PubMed Central PMCID: PMC4483048.