4'C-Ethynyl-thymidine acts as a chain terminator during DNA-synthesis catalyzed by HIV-1 reverse transcriptase

Summerer, Daniel; Marx, Andreas

4'C-Ethynyl-thymidine acts as a chain terminator during DNA-synthesis catalyzed by HIV-1 reverse transcriptase

Files

Summerer.pdf(9.91 MB)

Date

2005

Publication type

Journal article

Published in

Bioorganic & Medicinal Chemistry Letters ; 15 (2005), 4. - pp. 869-871. - ISSN 0960-894X

Abstract

Recently, 4'C-ethynyl nucleoside analogues have been identified as highly potent agents against HIV-1, including several multidrug-resistant strains. In contrast to most known nucleoside inhibitors 4'C-ethynyl nucleoside analogues possess a 3'-hydroxyl function. Here we show that the 5'O-triphosphate of 4'C-ethynyl thymidine gets readily incorporated into a nascent DNA strand by HIV-1 reverse transcriptase and significantly inhibits further post-incorporation chain extension by the enzyme.

Subject (DDC)

540 Chemistry

Cite This

ISO 690

SUMMERER, Daniel, Andreas MARX, 2005. 4'C-Ethynyl-thymidine acts as a chain terminator during DNA-synthesis catalyzed by HIV-1 reverse transcriptase. In: Bioorganic & Medicinal Chemistry Letters. 15(4), pp. 869-871. ISSN 0960-894X. Available under: doi: 10.1016/j.bmcl.2004.12.072

BibTex

@article{Summerer2005-02-154CEth-434,
  year={2005},
  doi={10.1016/j.bmcl.2004.12.072},
  title={4'C-Ethynyl-thymidine acts as a chain terminator during DNA-synthesis catalyzed by HIV-1 reverse transcriptase},
  number={4},
  volume={15},
  issn={0960-894X},
  journal={Bioorganic & Medicinal Chemistry Letters},
  pages={869--871},
  author={Summerer, Daniel and Marx, Andreas}
}

RDF

<rdf:RDF
    xmlns:dcterms="http://purl.org/dc/terms/"
    xmlns:dc="http://purl.org/dc/elements/1.1/"
    xmlns:rdf="http://www.w3.org/1999/02/22-rdf-syntax-ns#"
    xmlns:bibo="http://purl.org/ontology/bibo/"
    xmlns:dspace="http://digital-repositories.org/ontologies/dspace/0.1.0#"
    xmlns:foaf="http://xmlns.com/foaf/0.1/"
    xmlns:void="http://rdfs.org/ns/void#"
    xmlns:xsd="http://www.w3.org/2001/XMLSchema#" > 
  <rdf:Description rdf:about="https://kops.uni-konstanz.de/server/rdf/resource/123456789/434">
    <dc:contributor>Summerer, Daniel</dc:contributor>
    <dc:rights>terms-of-use</dc:rights>
    <dc:creator>Marx, Andreas</dc:creator>
    <foaf:homepage rdf:resource="http://localhost:8080/"/>
    <bibo:uri rdf:resource="http://kops.uni-konstanz.de/handle/123456789/434"/>
    <dcterms:available rdf:datatype="http://www.w3.org/2001/XMLSchema#dateTime">2011-07-01T10:08:56Z</dcterms:available>
    <dcterms:title>4'C-Ethynyl-thymidine acts as a chain terminator during DNA-synthesis catalyzed by HIV-1 reverse transcriptase</dcterms:title>
    <dc:format>application/pdf</dc:format>
    <dc:language>eng</dc:language>
    <dspace:isPartOfCollection rdf:resource="https://kops.uni-konstanz.de/server/rdf/resource/123456789/52"/>
    <dc:creator>Summerer, Daniel</dc:creator>
    <void:sparqlEndpoint rdf:resource="http://localhost/fuseki/dspace/sparql"/>
    <dcterms:isPartOf rdf:resource="https://kops.uni-konstanz.de/server/rdf/resource/123456789/52"/>
    <dc:date rdf:datatype="http://www.w3.org/2001/XMLSchema#dateTime">2011-07-01T10:08:56Z</dc:date>
    <dspace:hasBitstream rdf:resource="https://kops.uni-konstanz.de/bitstream/123456789/434/1/Summerer.pdf"/>
    <dcterms:hasPart rdf:resource="https://kops.uni-konstanz.de/bitstream/123456789/434/1/Summerer.pdf"/>
    <dcterms:issued>2005-02-15</dcterms:issued>
    <dcterms:rights rdf:resource="https://rightsstatements.org/page/InC/1.0/"/>
    <dc:contributor>Marx, Andreas</dc:contributor>
    <dcterms:abstract xml:lang="eng">Recently, 4'C-ethynyl nucleoside analogues have been identified as highly potent agents against HIV-1, including several multidrug-resistant strains. In contrast to most known nucleoside inhibitors 4'C-ethynyl nucleoside analogues possess a 3'-hydroxyl function. Here we show that the 5'O-triphosphate of 4'C-ethynyl thymidine gets readily incorporated into a nascent DNA strand by HIV-1 reverse transcriptase and significantly inhibits further post-incorporation chain extension by the enzyme.</dcterms:abstract>
    <dcterms:bibliographicCitation>First publ. in: Bioorganic &amp; medicinal chemistry letters 15 (2005), 4, pp. 869-871</dcterms:bibliographicCitation>
  </rdf:Description>
</rdf:RDF>

Bibliography of Konstanz

Yes