Linked Life Data

10799837

Source:http://linkedlifedata.com/resource/pubmed/id/10799837

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
2000-7-7
pubmed:abstractText
This review summarises the evidence for the potential antineoplastic activity of the staurosporine analogues 7-hydroxystaurospine (UCN-01) and N-benzoylstaurosporine (CGP 41251) and defines the role of the enzyme family protein kinase C (PKC) in the mechanisms by which these agents interfere with malignant cell growth. PKC function is altered in some neoplasias, and this dysfunction has been related to uncontrolled proliferation. PKC also influences resistance of cancer cells against cytotoxic drugs. Staurosporine analogues compete with ATP, even though the exact action by which they inhibit PKC is more complicated. Staurosporine analogues do not exhibit specificity for particular PKC isoenzymes, but they inhibit 'conventional' PKC isoenzymes more potently than 'novel' and 'atypical' ones. They also interfere directly with the cell cycle machinery. Both CGP 41251 and UCN-01 are currently progressing through clinical evaluation. There is a remarkable difference in pharmacokinetic handling of CGP 41251 and UCN-01 between rodents and humans. CGP 41251 and UCN-01 might offer advantages in cancer therapy when applied in combination with conventional cytotoxic agents.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
May
pubmed:issn
1040-8428
pubmed:author
pubmed:issnType
Print
pubmed:volume
34
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
127-35
pubmed:dateRevised
2007-11-15
pubmed:meshHeading
pubmed:year
2000
pubmed:articleTitle
Staurosporine analogues - pharmacological toys or useful antitumour agents?
pubmed:affiliation
Medical Research Council Toxicology Unit, Centre for Mechanisms of Human Toxicity, University of Leicester, Lancaster Road, PO Box 138, Leicester, UK.
pubmed:publicationType
Journal Article, Review