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• W2107067138 abstract "The dimerization initiation site (DIS) of the HIV-1 genomic RNA is a conserved stem-loop that promotes viral genome dimerization by forming a loop-loop complex. The DIS constitutes a potentially interesting target because it is crucial for several key steps of the viral replication. In this work we describe the synthesis of a rationally designed aminoglycoside conjugate that binds the HIV-1 DIS viral RNA with high specificity, as shown by an extensive in vitro binding characterization. We propose a three-dimensional model of the drug-RNA interaction that perfectly fits with binding data. Our results show the feasibility of targeting the HIV DIS viral RNA dimer and open the way to the rationale design of a new class of antiviral drugs. In addition, due to similarities between the HIV-1 DIS RNA and the bacterial aminoacyl decoding site (A site) RNA, we show that this novel aminoglycoside conjugate also binds the bacterial A site with a similar affinity as natural aminoglycoside antibiotics." @default.
• W2107067138 created "2016-06-24" @default.
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• W2107067138 date "2013-09-20" @default.
• W2107067138 modified "2023-10-05" @default.
• W2107067138 title "Structure-Guided Discovery of a Novel Aminoglycoside Conjugate Targeting HIV-1 RNA Viral Genome" @default.
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• W2107067138 doi "https://doi.org/10.1021/cb400498n" @default.
• W2107067138 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/24015986" @default.
• W2107067138 hasPublicationYear "2013" @default.
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