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

作者信息

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

机构信息

Shibaura Institute of Technology, Department of Applied Chemistry, Toyosu 3-7-5, Koto-ku, Tokyo 138-8548, Japan.

Shibaura Institute of Technology, Department of Applied Chemistry, Toyosu 3-7-5, Koto-ku, Tokyo 138-8548, Japan.

出版信息

Bioorg Med Chem. 2015 May 1;23(9):2139-47. doi: 10.1016/j.bmc.2015.03.001. Epub 2015 Mar 7.

DOI:10.1016/j.bmc.2015.03.001
PMID:25819332
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.

摘要

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