Linked Life Data

2441029

Source:http://linkedlifedata.com/resource/pubmed/id/2441029

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1
pubmed:dateCreated
1987-8-31
pubmed:abstractText
The new adriamycin (ADR) derivatives, 3'-deamino-3'-(4"-morpholinyl)adriamycin (MRA) and 3'-deamino-3'-(3"-cyano-4"-morpholinyl)-adriamycin (MRA-CN), were studied, in comparison with ADR, for their inhibitory effects on DNA and RNA syntheses in vitro using isolated DNA and RNA polymerases from both Escherichia coli and chicken (myeloblastosis) leukemia cells. Under standard assay conditions, MRA and ADR demonstrated a similar inhibitory effect on the enzymes, whereas MRA-CN showed a slightly greater inhibitory activity than ADR or MRA at low drug concentrations, but with the inhibitory effect plateauing when drug concentration reached 10 microM. Both the A and B forms of the MRA-CN diastereoisomers were effective as inhibitors. Kinetic studies of the inhibition showed that unlike ADR, MRA-CN inhibition of DNA or RNA synthesis could not be reversed by increasing DNA-template concentration in the reaction mixture. Whereas ADR or MRA relaxed completely 1 microgram of pBR322 supercoiled DNA at a drug concentration of 15 microM, MRA-CN, at 60 microM, produced a mixture of intermediate relaxation forms of the DNA. A complete relaxation was achieved at 300 microM MRA-CN. Both DNA relaxation and fluorescence spectroscopic studies indicated that DNA-drug interactions occurred in the following order: ADR (or MRA) greater than MRA-CN greater than N-trifluoroacetyl-ADR-14-O-hemiadipate (a DNA-nonbinding anthracycline).
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jul
pubmed:issn
0022-3565
pubmed:author
pubmed:issnType
Print
pubmed:volume
242
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
372-7
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed:year
1987
pubmed:articleTitle
Effect of morpholinyladriamycin analogs and adriamycin on the activities of DNA polymerase alpha and RNA polymerase II of chicken leukemia cells.
pubmed:publicationType
Journal Article, Comparative Study, Research Support, U.S. Gov't, P.H.S.