Abstract:
:6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase isoform 3 (PFKFB3) is a key enzyme of the glycolytic pathway, and it plays an essential role in angiogenesis. 3-(3-Pyridinyl)-1-(4-pyridinyl)-2-propen-1-one (3PO) is frequently used as a glycolysis inhibitor and is thought to inhibit PFKFB3. However, this latter effect of 3PO has never been investigated in detail and was the aim of the present study. To demonstrate binding of 3PO to PFKFB3, we used isothermal titration calorimetry. However, 3PO did not bind to PFKFB3, even up to 750 µm, in contrast to 3 µm of AZ67, which is a potent and specific PFKFB3 inhibitor. Instead, 3PO accumulated lactic acid inside the cells, leading to a decrease in the intracellular pH and an inhibition of enzymatic reactions of the glycolytic pathway.
journal_name
FEBS Lettjournal_title
FEBS lettersauthors
Emini Veseli B,Perrotta P,Van Wielendaele P,Lambeir AM,Abdali A,Bellosta S,Monaco G,Bultynck G,Martinet W,De Meyer GRYdoi
10.1002/1873-3468.13878subject
Has Abstractpub_date
2020-09-01 00:00:00pages
3067-3075issue
18eissn
0014-5793issn
1873-3468journal_volume
594pub_type
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