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 | |
| 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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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