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

Emmanuel Riguet; Snehlata Tripathi; Binay Chaubey; Jérôme Désiré; Virendra N. Pandey; Jean Luc Décout

doi:10.1021/jm049642d

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

Emmanuel Riguet, Snehlata Tripathi, Binay Chaubey, Jérôme Désiré, Virendra N. Pandey, Jean Luc Décout

New Jersey Medical School (NJMS), Biochemistry

Research output: Contribution to journal › Article › peer-review

71 Scopus citations

Abstract

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.

Original language	English (US)
Pages (from-to)	4806-4809
Number of pages	4
Journal	Journal of medicinal chemistry
Volume	47
Issue number	20
DOIs	https://doi.org/10.1021/jm049642d
State	Published - Sep 23 2004

All Science Journal Classification (ASJC) codes

Molecular Medicine
Drug Discovery

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10.1021/jm049642d

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abstract = "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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AU - Chaubey, Binay

AU - Désiré, Jérôme

AU - Pandey, Virendra N.

AU - Décout, Jean Luc

PY - 2004/9/23

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

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