The triazatruxene derivative azatrux binds to the parallel form of the human telomeric G-quadruplex under molecular crowding conditions: Biophysical and molecular modeling studies

Petraccone, L., Fotticchia, I., Cummaro, A., Pagano, B., Ginnari-Satriani, L., Haider, S.M., Randazzo, A., Novellino, E., Neidle, S. and Giancola, C. (2011) The triazatruxene derivative azatrux binds to the parallel form of the human telomeric G-quadruplex under molecular crowding conditions: Biophysical and molecular modeling studies. Biochimie, 93 (8). pp. 1318-1327. 10.1016/j.biochi.2011.05.017.

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DOI: 10.1016/j.biochi.2011.05.017

Abstract

The present study has employed a combination of spectroscopic, calorimetric and computational methods to explore the binding of the three side-chained triazatruxene derivative, termed azatrux, to a human telomeric G-quadruplex sequence, under conditions of molecular crowding. The binding of azatrux to the tetramolecular parallel [d(TGGGGT)]4 quadruplex in the presence and absence of crowding conditions, was also characterized. The data indicate that azatrux binds in an end-stacking mode to the parallel G-quadruplex scaffold and highlights the key structural elements involved in the binding. The selectivity of azatrux for the human telomeric G-quadruplex relative to another biologically relevant G-quadruplex (c-Kit87up) and to duplex DNA was also investigated under molecular crowding conditions, showing that azatrux has good selectivity for the human telomeric G-quadruplex over the other investigated DNA structures

Item Type:Article
Uncontrolled Keywords:Circular dichroism; G-quadruplex DNA; Isothermal titration calorimetry; Molecular crowding conditions; Molecular modeling; Quadruplex-ligand interaction
Departments, units and centres:Department of Pharmaceutical and Biological Chemistry > Centre for Pharmacognosy and Phytotherapy
ID Code:2733
Journal or Publication Title:Biochimie
Deposited By:Library Staff
Deposited On:20 Jan 2012 11:47
Last Modified:20 Jan 2012 11:47

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