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The synthesis of 2'-O-methyl G-clamp containing oligonucleotides and their inhibition of the HIV-1 Tat-TAR interaction.

作者信息

Holmes Stephen C, Gait Michael J

机构信息

Medical Research Council Laboratory of Molecular Biology, Cambridge, UK.

出版信息

Nucleosides Nucleotides Nucleic Acids. 2003 May-Aug;22(5-8):1259-62. doi: 10.1081/NCN-120022850.

DOI:10.1081/NCN-120022850
PMID:14565394
Abstract

We have synthesised a 2'-O-methyl riboside phosphoramidite derivative of the cytosine analogue 9-(2-aminoethoxy)-phenoxazine ('G-clamp') and successfully incorporated it into a series of small steric blocking 2'-O-methyl oligonucleotides targeting the stem-loop region of HIV-1 TAR RNA. The 'G-clamp' containing oligonucleotides show significant increases in binding to a model TAR RNA system when the 'G-clamp' is positioned opposite the loop region. The oligonucleotides also display dose-dependent inhibition of Tat-dependent transcription of an HIV DNA template in HeLa cell nuclear cell extract.

摘要

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