Journal
ANTICANCER RESEARCH
Volume 40, Issue 5, Pages 2613-2625Publisher
INT INST ANTICANCER RESEARCH
DOI: 10.21873/anticanres.14232
Keywords
Melanoma; BRAF(V600E); 3PO; A375; inhibitor; PFKFB3
Categories
Funding
- Statutory Funds of the Department of Molecular and Cellular Biology [SUB.D260.20.009]
- National Science Centre (Poland) [2016/22/E/NZ5/00671]
- Scientific Cancer Cell Biology Group [148]
- ERDF Project within the Innovation Economy Operational Programme [POIG.02.01.00-14-122/09]
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Background/Aim: The occurrence of BRAF(V600E) mutation causes an up-regulation of the B-raf kinase activity leading to the stabilization of hypoxia-inducible factor 1-alpha (HIF-1 alpha) - the promoter of the 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3) enzyme. The aim of the study was to examine the effect of the (2E)-3-(3-Pyridinyl)-1-(4-pyridinyl)-2-propen-1-one (3PO), as an inhibitor of PFKFB3, on human melanoma cells (A375) with endogenous BRAF(V600E) mutation. Materials and Methods: A375 cells were exposed to different concentrations of 3PO and the following tests were performed: docking, cytotoxicity assay, iminunocytochemistry staining glucose uptake, clonogenic assay, holotomography imaging, and flow cytometry. Results: Our studies revealed that 3PO presents a dose-dependent and time-independent cytotoxic effect and promotes apoptosis of A375 cells. Furthermore, the obtained data indicate that 3PO induces cell cycle arrest in G1/0 and glucose uptake reduction. Conclusion: Taking all together, our research demonstrated a here should be proapoptotic and antiproliferative effect of 3PO on A375 human melanoma cells.
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