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)
Bimolane
is a member of the bis(2,6-dioxopiperazine) class of drugs and has been widely used in China as an anti-neoplastic agent and for the treatment of psoriasis. Recent case reports indicate that bimolane is leukemogenic and is thought to exert its effects through the inhibition of
topoisomerase
II. However, there are no data showing the inhibition of
topoisomerase
II by this agent. In this report bimolane was shown to inhibit the activity of human
topoisomerase
II in vitro at concentrations of 100 microM and higher when pBR322 was used as the DNA substrate, whereas inhibition was seen at 1.5 mM when using kDNA as a substrate. The results of enzyme and DNA titration assays indicate that inhibition of
topoisomerase
II by bimolane occurred through interactions with DNA, similar to the mechanism seen with the epipodophyllotoxin-type inhibitors. These results provide evidence that bimolane is an inhibitor of
topoisomerase
II in vitro.
...
PMID:Bimolane: in vitro inhibitor of human topoisomerase II. 946 Oct 29
