Linked Life Data

20936822

Source:http://linkedlifedata.com/resource/pubmed/id/20936822

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
6
pubmed:dateCreated
2010-12-6
pubmed:abstractText
Before the active form of a Pt drug reaches its major pharmacological target in the cell nucleus, the Pt complex has to accumulate in cells, and during its transportation into cells and inside cells, it reacts with various biomolecules. Satraplatin is the first orally administered Pt drug under active clinical investigation. The major metabolite of this Pt(IV) complex is its Pt(II) analogue (JM118), which also has significant anticancer properties. Here we report the role of active transport in cellular entry of satraplatin and JM118 and interactions of these Pt complexes with glutathione. The results reveal that the organic cation transporters may play a more important role in the mechanism of cytotoxicity of JM118 than in the cytotoxicity of cisplatin. In contrast, satraplatin is a poor substrate of these transporters. In addition, satraplatin reacts with glutathione with the rate markedly lower than JM118 and cisplatin. Interestingly, satraplatin can be activated by glutathione allowing it to react with DNA, although to a much lower extent than in the case of another Pt(IV) drug tetraplatin.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Dec
pubmed:issn
1543-8392
pubmed:author
pubmed:issnType
Electronic
pubmed:day
6
pubmed:volume
7
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
2093-102
pubmed:meshHeading
pubmed:year
2010
pubmed:articleTitle
Studies on cellular accumulation of satraplatin and its major metabolite JM118 and their interactions with glutathione.
pubmed:affiliation
Institute of Biophysics, Academy of Sciences of the Czech Republic, vvi, Kralovopolska 135, 612 65 Brno, Czech Republic.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't