Hydroxyl-Functionalized DNAs with Different Linkers and Their Complmentary Duplex Stability

Zhang, Di; Li, Yamin; Xu, Liang; Cheng, Maosheng; He, Junlin; Liu, Keliang

doi:10.1080/15257770.2010.510124

Cited by 5 publications

(3 citation statements)

References 16 publications

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“…1-Palmitoyl-2-oleoyl-snglycero-3-phosphocholine (POPC) was purchased from Avanti Polar Lipids (Alabaster, AL). Phosphoramidites of deoxynucleotides 1, 2, and 3 were synthesized as previously described (27,28). 1H, 13C, and 31P nu-clear magnetic resonance (NMR) data were recorded on a JNM-ECA-400 spectrometer (JEOL, Japan).…”

Section: Methodsmentioning

confidence: 99%

“…1, panels 1 to 3) containing hydrophobic groups at the base site were generated via de novo synthesis as previously described (27,28) and used in this study as a means of maintaining a balance between hydrophobic and charged groups within the modified DNA duplexes. As these nucleoside analogues could be designed either at the end or in the middle of the duplexes, along with the 5= hydroxyl end, several combinations of hydrophobic groups could be realized.…”

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confidence: 99%

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DNA Duplexes with Hydrophobic Modifications Inhibit Fusion between HIV-1 and Cell Membranes

Xu¹,

Cai²,

Chen

et al. 2013

Antimicrob Agents Chemother

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Discovery of new drugs for the treatment of AIDS typically possessing unique structures associated with novel mechanisms of action has been of great importance due to the quick drug-resistant mutations of HIV-1 strains. The work presented in this report describes a novel class of DNA duplex-based HIV-1 fusion inhibitors. Hydrophobic groups were introduced into a DNA duplex skeleton either at one end, at both ends, or in the middle. These modified DNA duplexes inhibited fusion between HIV-1 and human cell membranes at micro-or submicromolar concentrations. Respective inhibitors adopted an aptamer pattern instead of a base-pairing interaction pattern. Structure-activity relationship studies of the respective DNA duplexes showed that the rigid and negatively charged DNA skeletons, in addition to the presence of hydrophobic groups, were crucial to the anti-HIV-1 activity of these compounds. A fluorescent resonance energy transfer (FRET)-based inhibitory assay showed that these duplex inhibitors interacted with the primary pocket in the gp41 N-terminal heptad repeat (NHR) instead of interacting with the lipid bilayers.

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Section: Methodsmentioning

confidence: 99%

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confidence: 99%