Probing the Importance of the G-Quadruplex Grooves for the Activity of the Anti-HIV-Integrase Aptamer T30923
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 groo...
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| Format: | Article |
| Language: | English |
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MDPI AG
2020-08-01
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| Series: | International Journal of Molecular Sciences |
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| Online Access: | https://www.mdpi.com/1422-0067/21/16/5637 |
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| author | Veronica Esposito Francesca Esposito Antonietta Pepe Isabel Gomez Monterrey Enzo Tramontano Luciano Mayol Antonella Virgilio Aldo Galeone |
| author_facet | Veronica Esposito Francesca Esposito Antonietta Pepe Isabel Gomez Monterrey Enzo Tramontano Luciano Mayol Antonella Virgilio Aldo Galeone |
| author_sort | Veronica Esposito |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-03-10T17:53:16Z |
| format | Article |
| id | doaj.art-ce32a1bcec984cdaad90444946aba7e3 |
| institution | Directory Open Access Journal |
| issn | 1661-6596 1422-0067 |
| language | English |
| last_indexed | 2024-03-10T17:53:16Z |
| publishDate | 2020-08-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | International Journal of Molecular Sciences |
| spelling | doaj.art-ce32a1bcec984cdaad90444946aba7e32023-11-20T09:17:44ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672020-08-012116563710.3390/ijms21165637Probing the Importance of the G-Quadruplex Grooves for the Activity of the Anti-HIV-Integrase Aptamer T30923Veronica Esposito0Francesca Esposito1Antonietta Pepe2Isabel Gomez Monterrey3Enzo Tramontano4Luciano Mayol5Antonella Virgilio6Aldo Galeone7Department of Pharmacy, University of Naples Federico II, 80131 Napoli, ItalyDepartment of Life and Environmental Sciences, University of Cagliari, Cittadella Universitaria SS554, 09045 Monserrato (CA), ItalyDepartment of Science, University of Basilicata, 85100 Potenza, ItalyDepartment of Pharmacy, University of Naples Federico II, 80131 Napoli, ItalyDepartment of Life and Environmental Sciences, University of Cagliari, Cittadella Universitaria SS554, 09045 Monserrato (CA), ItalyDepartment of Pharmacy, University of Naples Federico II, 80131 Napoli, ItalyDepartment of Pharmacy, University of Naples Federico II, 80131 Napoli, ItalyDepartment of Pharmacy, University of Naples Federico II, 80131 Napoli, ItalyIn 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.https://www.mdpi.com/1422-0067/21/16/5637G-quadruplex8-methyl-2′-deoxyguanosineaptamersintegraseHIV |
| spellingShingle | Veronica Esposito Francesca Esposito Antonietta Pepe Isabel Gomez Monterrey Enzo Tramontano Luciano Mayol Antonella Virgilio Aldo Galeone Probing the Importance of the G-Quadruplex Grooves for the Activity of the Anti-HIV-Integrase Aptamer T30923 International Journal of Molecular Sciences G-quadruplex 8-methyl-2′-deoxyguanosine aptamers integrase HIV |
| title | Probing the Importance of the G-Quadruplex Grooves for the Activity of the Anti-HIV-Integrase Aptamer T30923 |
| title_full | Probing the Importance of the G-Quadruplex Grooves for the Activity of the Anti-HIV-Integrase Aptamer T30923 |
| title_fullStr | Probing the Importance of the G-Quadruplex Grooves for the Activity of the Anti-HIV-Integrase Aptamer T30923 |
| title_full_unstemmed | Probing the Importance of the G-Quadruplex Grooves for the Activity of the Anti-HIV-Integrase Aptamer T30923 |
| title_short | Probing the Importance of the G-Quadruplex Grooves for the Activity of the Anti-HIV-Integrase Aptamer T30923 |
| title_sort | probing the importance of the g quadruplex grooves for the activity of the anti hiv integrase aptamer t30923 |
| topic | G-quadruplex 8-methyl-2′-deoxyguanosine aptamers integrase HIV |
| url | https://www.mdpi.com/1422-0067/21/16/5637 |
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