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

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.

journal_name

Biochimie

journal_title

Biochimie

authors

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

doi

10.1016/j.biochi.2011.05.017

subject

Has Abstract

pub_date

2011-08-01 00:00:00

pages

1318-27

issue

8

eissn

0300-9084

issn

1638-6183

pii

S0300-9084(11)00174-X

journal_volume

93

pub_type

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