Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1
pubmed:dateCreated
1999-11-22
pubmed:abstractText
A novel inhibitor of topoisomerases designated as Macrostatin has been isolated from the culture filtrate of Streptomyces avermitilis strain No. C-127 and purified by successive chromatography on Dowex, activated charcoal, gel filtration and cellulose. It is an acidic macromolecule having 45 kD molecular weight as determined by gel filtration. Macrostatin inhibited topoisomerase I and II in a noncompetitive manner with Ki = 3.7 and 1.3 nM respectively. Macrostatin differed from well-known inhibitors of topoisomerase such as camptothecin, etoposide and doxorubicin which induce topoisomerase-mediated DNA cleavage by stabilizing the cleavable complex or intercalation into DNA strands. Macrostatin had neither ability to stabilize the cleavable complex nor ability to intercalate into DNA strands. It was suggested that Macrostatin inhibits topoisomerase by a direct action on the enzyme.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
8755-5093
pubmed:author
pubmed:issnType
Print
pubmed:volume
14
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
69-83
pubmed:dateRevised
2010-11-18
pubmed:meshHeading
pubmed:year
1998
pubmed:articleTitle
Macrostatin, a novel macromolecular inhibitor of topoisomerases produced by Streptomyces avermitilis no. C-127.
pubmed:affiliation
Faculty of Pharmaceutical Sciences, Kumamoto University, Japan.
pubmed:publicationType
Journal Article, Comparative Study