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OLIGONUCLEOTIDE ANALOGUE INTERFERENCE WITH THE HIV-1 TAT PROTEIN-TAR RNA INTERACTION.
In: Nucleosides, Nucleotides & Nucleic Acids, Jg. 20 (2001-04-01), Heft 4-7, S. 471-480
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Zugriff:
The HIV-1 Tat protein interaction with its RNA recognition sequence TAR is an important drug target and model system for the development of specific RNA-protein inhibitors. 2′-O-methyl oligoribonucleotides complementary to the TAR apical stem-loop effectively block Tat binding in vitro. Substitution by 5-propynylC or 5-methylC LNA monomeric units into a 12-mer 2′-O-methyl oligoribonucleotide leads to stronger inhibition, as does a 12-mer PNA. 10–16 mer 2′-O-methyl oligoribonucleotides give sequence- and dose-dependent inhibition of Tat-dependent transcription of an HIV DNA template in HeLa cell nuclear extract. Inhibition is maintained for the substituted 12-mer analogues but is poorer for PNA and is not correlated with TAR binding strength. [ABSTRACT FROM AUTHOR]
Titel: |
OLIGONUCLEOTIDE ANALOGUE INTERFERENCE WITH THE HIV-1 TAT PROTEIN-TAR RNA INTERACTION.
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Autor/in / Beteiligte Person: | Arzumanov, Andrey ; Walsh, AndrewP. ; Liu, Xiaohai ; Rajwanshi, VivekK. ; Wengel, Jesper ; Gait, MichaelJ. |
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Zeitschrift: | Nucleosides, Nucleotides & Nucleic Acids, Jg. 20 (2001-04-01), Heft 4-7, S. 471-480 |
Veröffentlichung: | 2001 |
Medientyp: | academicJournal |
ISSN: | 1525-7770 (print) |
DOI: | 10.1081/NCN-100002321 |
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