Abstract
LNA and alpha-L-LNA are promising candidates for the development of efficient oligonucleotide-based therapeutic agents. Here, we report dose-dependent inhibition of HIV-1 Tat-dependent trans activation by a 12-mer chimeric alpha-L-LNA/DNA oligomer. This oligomer exhibits a dose-dependency similar to that of the corresponding 12-mer chimeric LNA/2'-O-Me-RNA oligomer. In addition, we show that incorporation of alpha-L-LNA or LNA monomers into each of the two binding arms of a "10-23" DNAzyme markedly increases cleavage of the target RNA.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Base Sequence
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Chimera
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DNA, Catalytic / metabolism
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Gene Products, tat / metabolism
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HIV-1 / drug effects
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HIV-1 / genetics
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Nucleic Acid Conformation
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Oligonucleotides
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Oligonucleotides, Antisense / chemistry*
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Oligonucleotides, Antisense / therapeutic use*
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Transcriptional Activation
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tat Gene Products, Human Immunodeficiency Virus
Substances
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DNA, Catalytic
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Gene Products, tat
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Oligonucleotides
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Oligonucleotides, Antisense
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locked nucleic acid
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tat Gene Products, Human Immunodeficiency Virus