PFKFB3

Supporting information

PFKFB3 (6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase-3) is an enzyme that plays a key role in the regulation of glycolysis in rapidly dividing cells, so is important in cancer metabolism and during development. PFKFB3 is present in a wide variety of tissues and is induced under hypoxic conditions. The enzyme is one of four PFKFB isozymes and differs from other family members in that it has a very high kinase:phosphatase activity ratio and is overexpressed in a range of cancer types. It is important in the maintenance of fructose-2,6-bisphosphate (F2,6BP) levels in cells, which is an activator of 6-phosphofructo-1-kinase, a rate-limiting enzyme in glycolysis. It has been shown that inhibition of PFKFB3 reduces intracellular F2,6BP levels and suppresses glucose uptake and glycolysis.

PFKFB3 is also a substrate for APC/C (anaphase-promoting complex/cyclosome)-Cdh1, a ubiquitin ligase that controls progression along the cell cycle from G1- to S-phase. The inactivation of APC/C -Cdh1 during mid-to-late G1 results in a rise in PFKFB3 levels and a transient increase in lactate generation. Therefore the presence of PFKFB3 at this particular stage of the cell cycle ensures the upregulation of glycolysis and the provision of sufficient nutrients for cell division.

In addition, F2,6BP activates certain cyclin dependent kinases; in particular, it promotes the Cdk-mediated phosphorylation of p27. p27 has an important role in cell cycle regulation, suppressing transition from G1- to S-phase and promoting apoptosis. Phosphorylation of p27, however, leads to its ubiquitination and proteasomal degradation. So increased F2,6BP levels associated with upregulation of PFKFB3, as seen in cancerous cells, are associated with cell proliferation and inhibition of apoptosis.

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Gene Species Gene Symbol Gene Accession No. Protein Accession No.
PFKFB3 Human PFKFB3 NM_004566 Q16875
Mouse Pfkfb3 NM_001177753 A7UAK5
Rat Pfkfb3 NM_057135 NP_476476

Literature for PFKFB3

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