4.7 Article

A peptide nucleic acid-neamine conjugate that targets and cleaves HIV-1 TAR RNA inhibits viral replication

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JOURNAL OF MEDICINAL CHEMISTRY
卷 47, 期 20, 页码 4806-4809

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AMER CHEMICAL SOC
DOI: 10.1021/jm049642d

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  1. NIAID NIH HHS [AI42520] Funding Source: Medline

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The neamine part of the aminoglycoside antibiotic neomycin B was conjugated to a 16 mer peptide nucleic acid (PNA) targeting HIV-1 TAR RNA. Attachment of the neamine core allows cellular uptake of the PNA and results in potent inhibition of HIV-1 replication. The polycationic neamine moiety imparts greater solubility to the PNA and also confers a unique RNA cleavage property to the conjugate which is specific to its target site and functional at physiological concentrations of Mg2+. These properties suggest a potential therapeutic application for this class of compounds.

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