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Literature summary for 3.5.1.2 extracted from

  • Xie, C.; Jin, J.; Bao, X.; Zhan, W.H.; Han, T.Y.; Gan, M.; Zhang, C.; Wang, J.
    Inhibition of mitochondrial glutaminase activity reverses acquired erlotinib resistance in non-small cell lung cancer (2016), Oncotarget, 7, 610-621 .
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
medicine strategy to overcome acquired erlotinib resistance in NSCLC by inhibiting glutaminase activity. Compound 968, an inhibitor of the glutaminase C, when combined with erlotinib potently inhibits the cell proliferation of erlotinib-resistant NSCLC cells HCC827ER and NCI-H1975. The combination of compound 968 and erlotinib decreases glutaminase C and EGFR protein expression and inhibits glutaminase C activity in HCC827ER cells. Compound 968 combined with erlotinib down-regulates the glutamine and glycolysis metabolism in erlotinib-resistant cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
compound 968 i.e. 5-(3-bromo-4-(dimethylamino)phenyl)-2,2-dimethyl-2,3,5,6-tetrahydrobenzo[a]phenanthridin-4(1H)-one, combined with erlotinib down-regulates the glutamine and glycolysis metabolism in erlotinib-resistant non-small cell lung cancer cells Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
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Source Tissue

Source Tissue Comment Organism Textmining
HCC-827 cell
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Homo sapiens
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