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

L. Petraccone, I. Fotticchia, A. Cummaro, B. Pagano, L. Ginnari-Satriani, Shozeb Haider, A. Randazzo, E. Novellino, S. Neidle, C. Giancola

Research output: Contribution to journalArticlepeer-review

31 Citations (Scopus)

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. (C) 2011 Elsevier Masson SAS. All rights reserved.
Original languageEnglish
Pages (from-to)1318-1327
Number of pages10
JournalBiochimie
Volume93
Issue number8
DOIs
Publication statusPublished - Aug 2011

ASJC Scopus subject areas

  • Biochemistry

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