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

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

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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

Cite this

Inoue, R., Watanabe, K., Katou, T., Ikezawa, Y., & Hamasaki, K. (2015). Nucleobase modified neamines with a lysine as a linker, their inhibition specificity for TAR-Tat derived from HIV-1. Bioorganic and Medicinal Chemistry, 23(9), 2139-2147. https://doi.org/10.1016/j.bmc.2015.03.001

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AU - Hamasaki, Keita

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10.1016/j.bmc.2015.03.001