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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
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pubmed:dateCreated |
1998-10-30
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pubmed:abstractText |
Thymidine-5'-fluorothiophosphate, dTMP(S)-F, was synthesized by the oxathiaphospholane, and thymidine 5'-dithiophosphate, dTMPS2, by the dithiaphospholane, method. To estimate the role of 5'-phosphate group ionization in binding of pyrimidine nucleotides by thymidylate synthase, dTMP(S)-F was studied as an inhibitor of mouse tumour (L1210) enzyme, and its inhibitory properties were compared with those of dTMPS2, a close dTMP analogue. While dTMPS2 proved to be an inhibitor, competitive vs dUMP, with K(i)app = 94 microM, the 5'-fluorothiophosphate congener displayed no activity, indicating that the enzyme requires for binding the presence of a dianionic 5'-phosphate group in a nucleotide.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:issn |
0001-527X
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
45
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
83-6
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:9701499-Animals,
pubmed-meshheading:9701499-Drug Screening Assays, Antitumor,
pubmed-meshheading:9701499-Enzyme Inhibitors,
pubmed-meshheading:9701499-Leukemia L1210,
pubmed-meshheading:9701499-Mice,
pubmed-meshheading:9701499-Thiophosphoric Acid Esters,
pubmed-meshheading:9701499-Thymidylate Synthase
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pubmed:year |
1998
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pubmed:articleTitle |
Synthesis and interaction with thymidylate synthase of 5'-dithiophosphate and 5'-fluorothiophosphate of thymidine.
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pubmed:affiliation |
Nencki Institute of Experimental Biology, Polish Academy of Sciences, Warsaw.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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