Organic & Biomolecular Chemistry · 2003 · 25 citations · 32 references
PharmacyMedicinal ChemistryMolecular BiologyDrug DesignDrug DiscoveryMolecular VirologyAntiviral PharmacologyRibonucleic Acid (Rna) ChemistryRna ChemistryRna StructureViral Rna BiologyViral StructureAntisense RnasAntiviral Drug DesignAntiviral Structure-activity RelationshipsLiquid-phase ReactionsNucleoside AnalogsNucleoside Reverse Transcriptase InhibitorsPna Synthesis
A cyclic molecule including a hexameric PNA sequence has been designed and synthesized in order to target the TAR RNA loop of HIV-1 through the formation of a "kissing complex". For comparison, its linear analogue has also been investigated. The synthesis of the cyclic and linear PNA has been accomplished following a liquid-phase strategy using mixed PNA and fully N-protected (aminoethylglycinamide) fragments. The interactions of this cyclic PNA and its linear analogue with TAR RNA have been studied and the results indicate clearly that no interaction occurs between the cyclic antisense PNA and TAR RNA, whereas a tenuous interaction has been detected with its linear PNA analogue.
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