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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
5
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pubmed:dateCreated |
1991-2-26
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pubmed:abstractText |
PTT-119 is an antineoplastic agent in which an alkylating moiety, m-sarcolysine, is linked to two amino acid analogs. Previous studies showed a higher "in vitro" cytotoxicity of PTT-119 when compared to free m-sarcolysine; the mechanisms of this enhanced activity are not completely understood. In this study we incubated peripheral blood cells from 8 chronic lymphocytic leukemia patients with both m-sarcolysine and equimolar concentrations of PTT-119, measuring the intracellular concentration of the alkylating moiety. We observed a significantly higher intracellular concentration of m-sarcolysine in cells incubated with the peptide-bound drug than with the free drug (58.3 +/- 39.6 versus 4.4 +/- 1.9 ng/10(6) cells; P = 0.013). This observation could explain the higher cytotoxic activity of PTT-119 and the lack of cross-resistance with melphalan.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Amino Acids,
http://linkedlifedata.com/resource/pubmed/chemical/Drug Combinations,
http://linkedlifedata.com/resource/pubmed/chemical/Melphalan,
http://linkedlifedata.com/resource/pubmed/chemical/Nitrogen Mustard Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/ambamustine
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
0006-5242
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pubmed:author | |
pubmed:issnType |
Print
|
pubmed:volume |
61
|
pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
|
pubmed:pagination |
311-3
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:2271778-Amino Acids,
pubmed-meshheading:2271778-Biological Transport,
pubmed-meshheading:2271778-Drug Combinations,
pubmed-meshheading:2271778-Humans,
pubmed-meshheading:2271778-Intracellular Membranes,
pubmed-meshheading:2271778-Melphalan,
pubmed-meshheading:2271778-Nitrogen Mustard Compounds,
pubmed-meshheading:2271778-Osmolar Concentration
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pubmed:year |
1990
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pubmed:articleTitle |
Evidence for increased intracellular transport of m-sarcolysine (alkylating moiety) when combined with two amino acid analogs (PTT-119).
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pubmed:affiliation |
L. e A. Seràgnoli Haematology Institute, University of Bologna, Italy.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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