Preferred Label : Pyruvate Kinase M2 Isoform Activator TP-1454;
NCIt synonyms : PKM2 Activator TP-1454;
NCIt definition : An orally bioavailable activator of pyruvate kinase M2 isoform (PKM2), with potential
immunomodulating and antineoplastic activities. Upon oral administration, PKM2 activator
TP-1454 locks PKM2 into the active tetrameric form. This may prevent the production
of glycolytic intermediates by the less active dimer form of PKM2, depleting the supply
of glycolytic intermediates which are needed for tumor cell growth. This may also
inhibit immune suppression mediated by the dimer form of PKM2. Altogether, this may
slow tumor cell growth and enhance anti-tumor immune responses, thereby inhibiting
tumor cell proliferation. PKM2, the predominant PK isoform found in tumor cells, is
responsible for catalyzing the last step of glycolysis. PKM2 plays a critical role
in the metabolic changes observed in cancer and immune cells and establishes a metabolic
advantage for tumor cells over the tumor immune microenvironment.;
Molecule name : TP-1454; TP 1454;
NCI Metathesaurus CUI : CL1412698;
Origin ID : C175380;
UMLS CUI : C5446478;
Semantic type(s)
- concept_is_in_subset
- has_target
