1. Evaluation of neomycin analogues for HIV-1 RRE RNA recognition identifies enhanced activity simplified neamine analogues.
- Author
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Simon B, Walmsley C, Jackson VJ, Garvey EP, Slater MJ, Berrisford DJ, and Gardiner JM
- Subjects
- Anti-HIV Agents chemical synthesis, Anti-HIV Agents chemistry, Dose-Response Relationship, Drug, Framycetin chemical synthesis, Framycetin chemistry, Molecular Structure, Neomycin analogs & derivatives, Neomycin chemistry, Structure-Activity Relationship, Anti-HIV Agents pharmacology, Framycetin pharmacology, HIV-1 drug effects, Neomycin pharmacology, RNA, Viral drug effects, Response Elements drug effects
- Abstract
Synthetic neamine mimetics have been evaluated for binding to the HIV-1 Rev response element. Modified neamine derivatives, obtained from reductive amination of neamine, led to identification of new 6-amino modified neamine-type ligands with HIV-1 RRE binding affinity up to 20× that of neamine and up to 6× that of the more complex neomycin itself. This provides a noteworthy structure-activity increase and a useful lead to simplified, chemically accessible mimetics., (Copyright © 2018. Published by Elsevier Ltd.)
- Published
- 2019
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