Probing the Importance of the G-Quadruplex Grooves for the Activity of the Anti-HIV-Integrase Aptamer T30923.
Veronica EspositoFrancesca EspositoAntonietta PepeIsabel Gomez MonterreyEnzo TramontanoLuciano MayolAntonella VirgilioAldo GaleonePublished in: International journal of molecular sciences (2020)
In this paper, we report studies concerning four variants of the G-quadruplex forming anti-HIV-integrase aptamer T30923, in which specific 2'-deoxyguanosines have been singly replaced by 8-methyl-2'-deoxyguanosine residues, with the aim to exploit the methyl group positioned in the G-quadruplex grooves as a steric probe to investigate the interaction aptamer/target. Although, the various modified aptamers differ in the localization of the methyl group, NMR, circular dichroism (CD), electrophoretic and molecular modeling data suggest that all of them preserve the ability to fold in a stable dimeric parallel G-quadruplex complex resembling that of their natural counterpart T30923. However, the biological data have shown that the T30923 variants are characterized by different efficiencies in inhibiting the HIV-integrase, thus suggesting the involvement of the G-quadruplex grooves in the aptamer/target interaction.
Keyphrases
- antiretroviral therapy
- hiv positive
- hiv infected
- hiv testing
- gold nanoparticles
- human immunodeficiency virus
- sensitive detection
- hepatitis c virus
- hiv aids
- men who have sex with men
- magnetic nanoparticles
- label free
- electronic health record
- copy number
- south africa
- big data
- magnetic resonance
- high resolution
- signaling pathway
- single molecule
- mass spectrometry
- deep learning
- living cells
- gene expression
- dna methylation
- artificial intelligence
- nk cells