Kinetic ESI-MS Studies of Potent Anti-HIV Aptamers Based on the G-Quadruplex Forming Sequence d(TGGGAG)

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• 作者：Valeria Romanucci ; Adrien Marchand ; Oscar Mendoza ; Daniele D’Alonzo ; Armando Zarrelli ; Valérie Gabelica ; Giovanni Di Fabio
• 刊名：ACS Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：March 10, 2016
• 年：2016
• 卷：7
• 期：3
• 页码：256-260
• 全文大小：310K
• ISSN：1948-5875

文摘

To investigate what properties make tetramolecular G-quadruplex ODNs good anti-HIV aptamers, we studied the stoichiometry and the self-assembly kinetics of the highly active 5′-end modified G-quadruplexes based on the d(TGGGAG) sequence. Our results demonstrate that the 5′-end conjugation does not necessarily increase the folding rate of the G-quadruplex; indeed, it ascribes anti-HIV activity. Unexpectedly, the G4-folding kinetics of the inactive G4 is similar to that of the 5′-end modified sequences. ESI-MS studies also revealed the formation of higher order G4 structures identified as octameric complexes along with tetramolecular G-quadruplexes.