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