Preferred Label : OxPhos Inhibitor VLX600;
NCIt synonyms : 1-(2-Pyridinyl)ethanone(6-methyl-5H-[1,2,4]triazino[5,6-b]indol-3-yl)hydrazone;
NCIt related terms : VLX-600;
NCIt definition : A lipophilic cation-based triazinoindolyl-hydrazone compound and mitochondrial oxidative
phosphorylation (OxPhos) inhibitor, with potential antineoplastic activity. Upon infusion,
in normal cells and proliferating tumor cells where glucose is readily available,
inhibition of OxPhos by VLX600 induces a hypoxia-inducible factor 1-alpha (HIF-1alpha)-dependent
shift to, and an increase in glycolysis. Glycolysis alone does not produce enough
energy to support the growth of tumor cells in this environment, and the induction
of autophagy occurs. In the metabolically compromised tumor microenvironment, the
availability of oxygen and glucose is limited due to poor vascularization and perfusion
of tumor micro-areas. Tumor cells growing in this environment are thus unable to compensate
for decreased mitochondrial function by increasing glycolysis. This leads to nutrient
depletion, decreased energy production, induction of autophagy, tumor cell death and
an inhibition of cell proliferation in quiescent tumor cells. Mitochondrial OxPhos,
which is hyperactivated in cancer cells, plays a key role in the promotion of cancer
cell proliferation.;
UNII : YZO6DG19MG;
CAS number : 327031-55-0; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 327031-55-0
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G-SRS /a ;
Molecule name : VLX-600;
NCI Metathesaurus CUI : CL474135;
Origin ID : C118283;
UMLS CUI : C4078506;
Currated CISMeF NLP mapping
- VLX600 [MeSH Supplementary Concept]
- Semantic type(s)
- UMLS correspondences (same concept)
- VLX600 [MeSH Supplementary Concept]
- concept_is_in_subset
