skip navigation links
National Cancer Institute
EVS Logo NCI Term Browser Enterprise Vocabulary Services
Terminologies Value Sets Mappings
Version: 17.06d (Release date: 2017-06-26)
SearchBox Top
SearchBox Bottom
6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatases Isoform 3 Inhibitor ACT-PFK-158 (Code C113787)

Terms & Properties Synonym Details Relationships Mapping View All  
Terms & Properties

Preferred Name: 6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatases Isoform 3 Inhibitor ACT-PFK-158

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.

Label: 6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatases Isoform 3 Inhibitor ACT-PFK-158

NCI Thesaurus Code: C113787 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: CL471768  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatases Isoform 3 Inhibitor ACT-PFK-158
ACT-PFK-158
PFK-158
PFKFB3 Inhibitor PFK-158

External Source Codes: 
PDQ Closed Trial Search ID 757225
PDQ Open Trial Search ID 757225 (check for NCI PDQ open clinical trial info)
NCI META CUI CL471768

Other Properties:
     Name Value (qualifiers indented underneath)
code C113787
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  

URL: https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C113787

Mainbox Bottom