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Oxford University Press, Nucleic Acids Research, 20(39), p. 8984-8991, 2011

DOI: 10.1093/nar/gkr540

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HIV-1 integrase inhibitor T30177 forms a stacked dimeric G-quadruplex structure containing bulges

Journal article published in 2011 by Vineeth Thachappilly Mukundan, Ngoc Quang Do, Anh Tuân Phan ORCID
This paper is made freely available by the publisher.
This paper is made freely available by the publisher.

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Abstract

T30177 is a G-rich oligonucleotide with the sequence (GTGGTGGGTGGGTGGGT) which inhibits the HIV-1 integrase activity at nanomolar concentrations. Here we show that this DNA sequence forms in K+ solution a dimeric G-quadruplex structure comprising a total of six G-tetrad layers through the stacking of two propeller-type parallel-stranded G-quadruplex subunits at their 5′-end. All twelve guanines in the sequence participate in the G-tetrad formation, despite the interruption in the first G-tract by a thymine, which forms a bulge between two adjacent G-tetrads. In this work, we also propose a simple analytical approach to stoichiometry determination using concentration-dependent melting curves.