Nucleobase modified neamines with a lysine as a linker, their inhibition specificity for TAR-Tat derived from HIV-1

Ryo Inoue; Kentarou Watanabe; Toyofusa Katou; Yasunori Ikezawa; Keita Hamasaki

doi:10.1016/j.bmc.2015.03.001

Nucleobase modified neamines with a lysine as a linker, their inhibition specificity for TAR-Tat derived from HIV-1

Ryo Inoue, Kentarou Watanabe, Toyofusa Katou, Yasunori Ikezawa, Keita Hamasaki

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

7 Citations (Scopus)

Abstract

Nucleobase modified neamines with a lysine as the linker (NbK-neamines) were synthesized and their binding toward hairpin RNAs derived from HIV-1 activator region were studied. NbK-neamines were bind those RNAs with micro molar level of binding affinities and compete with corresponding activator peptide for TAR RNA, but not for RRE RNA. GbK-neamine denotes the highest binding affinity with TAR RNA, three to five times higher than other three NbK-neamines. GbK-neamine could be a candidate of potential inhibitor for TAR-Tat.

Original language	English
Pages (from-to)	2139-2147
Number of pages	9
Journal	Bioorganic and Medicinal Chemistry
Volume	23
Issue number	9
DOIs	https://doi.org/10.1016/j.bmc.2015.03.001
Publication status	Published - 2015 May 1

Keywords

Aminoglycoside
Neamine
Nucleobase
Potential inhibitor
RRE RNA
TAR RNA

ASJC Scopus subject areas

Biochemistry
Clinical Biochemistry
Molecular Biology
Molecular Medicine
Organic Chemistry
Drug Discovery
Pharmaceutical Science

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abstract = "Nucleobase modified neamines with a lysine as the linker (NbK-neamines) were synthesized and their binding toward hairpin RNAs derived from HIV-1 activator region were studied. NbK-neamines were bind those RNAs with micro molar level of binding affinities and compete with corresponding activator peptide for TAR RNA, but not for RRE RNA. GbK-neamine denotes the highest binding affinity with TAR RNA, three to five times higher than other three NbK-neamines. GbK-neamine could be a candidate of potential inhibitor for TAR-Tat.",

keywords = "Aminoglycoside, Neamine, Nucleobase, Potential inhibitor, RRE RNA, TAR RNA",

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AU - Inoue, Ryo

AU - Watanabe, Kentarou

AU - Katou, Toyofusa

AU - Ikezawa, Yasunori

AU - Hamasaki, Keita

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