Preferred Label : 6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatases Isoform 3 Inhibitor ACT-PFK-158;
NCIt synonyms : PFKFB3 Inhibitor PFK-158;
NCIt definition : An inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatases (PFK-2/FBPase)
isoform 3 (PFKFB3) and derivative of 3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one
(3PO), with potential antineoplastic activity. Upon administration, PFKFB3 inhibitor
PFK-158 binds to and inhibits the activity of PFKFB3, which leads to the inhibition
of both the glycolytic pathway in and glucose uptake by cancer cells. This prevents
the production of macromolecules and energy that causes the enhanced cellular proliferation
in cancer cells as compared to that of normal, healthy cells. Depriving cancer cells
of nutrients and energy leads to the inhibition of cancer cell growth. PFKFB3, an
enzyme that catalyzes the conversion of fructose-6-phosphate to fructose-2,6-bisphosphate,
is highly expressed and active in human cancer cells; it plays a key role in increasing
both glycolytic flux in and proliferation of cancer cells.;
Molecule name : PFK-158; ACT-PFK-158;
NCI Metathesaurus CUI : CL471768;
Origin ID : C113787;
UMLS CUI : C3827087;
Semantic type(s)
- UMLS correspondences (same concept)
- PFK158 [MeSH Supplementary Concept]
- concept_is_in_subset
