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Issue 6, 2016
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Multivalency in the recognition and antagonism of a HIV TAR RNA–TAT assembly using an aminoglycoside benzimidazole scaffold

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Abstract

Recognition of RNA by high-affinity binding small molecules is crucial for expanding existing approaches in RNA recognition, and for the development of novel RNA binding drugs. A novel neomycin dimer benzimidazole conjugate 5 (DPA 83) was synthesized by conjugating a neomycin-dimer with a benzimidazole alkyne using click chemistry to target multiple binding sites on HIV TAR RNA. Ligand 5 significantly enhances the thermal stability of HIV TAR RNA and interacts stoichiometrically with HIV TAR RNA with a low nanomolar affinity. 5 displayed enhanced binding compared to its individual building blocks including the neomycin dimer azide and benzimidazole alkyne. In essence, a high affinity multivalent ligand was designed and synthesized to target HIV TAR RNA.

Graphical abstract: Multivalency in the recognition and antagonism of a HIV TAR RNA–TAT assembly using an aminoglycoside benzimidazole scaffold

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Publication details

The article was received on 28 Sep 2015, accepted on 18 Dec 2015 and first published on 14 Jan 2016


Article type: Paper
DOI: 10.1039/C5OB02016F
Org. Biomol. Chem., 2016,14, 2052-2056

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    Multivalency in the recognition and antagonism of a HIV TAR RNA–TAT assembly using an aminoglycoside benzimidazole scaffold

    S. Kumar, N. Ranjan, P. Kellish, C. Gong, D. Watkins and D. P. Arya, Org. Biomol. Chem., 2016, 14, 2052
    DOI: 10.1039/C5OB02016F

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