Abstract
Manganese porphyrin-linker-triple-helix-forming oligonucleotide molecules were prepared and their ability to cleave in vitro a double-stranded DNA target present in the HIV-1 genome was studied. The nature of the linker is a determining factor of the cleavage efficiency. Cleavage yields as high as 80% were observed when the linker was a spermine residue and in the absence of a large excess of free spermine known to stabilize triplex structures. The hydrophobic nature of aliphatic diamine linker modified the cleaver-DNA interactions and reduced the efficiency of DNA cleavage.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antiviral Agents
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Base Sequence
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Cations, Divalent
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DNA Damage*
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DNA, Viral / metabolism*
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Drug Stability
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HIV-1 / genetics*
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Hot Temperature
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Magnesium / pharmacology
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Metalloporphyrins / chemistry
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Metalloporphyrins / metabolism*
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Molecular Sequence Data
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Molecular Structure
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Oligonucleotides / chemistry
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Oligonucleotides / metabolism*
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Sodium / pharmacology
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Spermine / chemistry
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Structure-Activity Relationship
Substances
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Antiviral Agents
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Cations, Divalent
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DNA, Viral
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Metalloporphyrins
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Oligonucleotides
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Spermine
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Sodium
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Magnesium