Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: EC:5.99.1.2 (
topoisomerase
)
9,166
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
The cytotoxic oxoaporphine alkaloid liriodenine, isolated from Cananga odorata, was found to be a potent inhibitor of
topoisomerase
II (EC 5.99.1.3) both in vivo and in vitro.
Liriodenine
treatment of SV40 (simian virus 40)-infected CV-1 cells caused highly catenated SV40 daughter chromosomes, a signature of
topoisomerase
II inhibition. Strong catalytic inhibition of
topoisomerase
II by liriodenine was confirmed by in vitro assays with purified human
topoisomerase
II and kinetoplast DNA.
Liriodenine
also caused low-level protein-DNA cross-links to pulse-labeled SV40 chromosomes in vivo, suggesting that it may be a weak
topoisomerase
II poison. This was supported by the finding that liriodenine caused
topoisomerase
II-DNA cross-links in an in vitro assay for
topoisomerase
II poisons. Verapamil did not increase either liriodenine-induced protein-DNA cross-links or catalytic inhibition of
topoisomerase
II in SV40-infected cells. This indicates that liriodenine is not a substrate for the verapamil-sensitive drug efflux pump in CV-1 cells.
...
PMID:Inhibition of topoisomerase II by liriodenine. 931 73
