NCIt definition : An orally bioavailable inhibitor of glutaminase, with potential antineoplastic activity.
Upon oral administration, CB-839 selectively and irreversibly inhibits glutaminase,
a mitochondrial enzyme that is essential for the conversion of the amino acid glutamine
into glutamate. By blocking glutamine utilization, proliferation in rapidly growing
cells is impaired. Glutamine-dependent tumors rely on the conversion of exogenous
glutamine into glutamate and glutamate metabolites to both provide energy and generate
building blocks for the production of macromolecules, which are needed for cellular
growth and survival.;
Semantic type(s)