G-quadruplex is a four-stranded DNA structure with large planar aromatic rings (G-quartet), potentially exists in human telomeres and it can inhibit telomerase activity.1 Telomerase is a promising target for cancer therapy because it plays a role in immortal cell growth by elongating telomere DNA.2 Therefore, ligands that can selectively stabilize GQs have attracted in recent years great interest as a promising new class of anticancer drugs. Many G-quadruplex-ligands contain a large π-planar core and cationic functional groups; these structures facilitate π–π stacking and electrostatic interactions toward GQ’s structures.3 Porphyrinoids are ideal compounds to interact with DNA due to their peculiar characteristics.4 It has been showed that cationic porphyrins have been utilized as reporters of different sequences and conformations of single and duplex DNA.5 We explored by CD, UV, FRET and melting experiments the different effects showed by a new cationic porphyrin bearing sperminate substituents, in the presence of different conformations of GQ obtained by models of G‐rich sequences (Tel22 and TG3AG).
Study of interactions between G‐quadruplex and porphyrin bearing sperminate substituents
GANGEMI, CHIARA MARIA ANTONIETTA;D'URSO, ALESSANDRO;TOMASELLI, Gaetano;
2014-01-01
Abstract
G-quadruplex is a four-stranded DNA structure with large planar aromatic rings (G-quartet), potentially exists in human telomeres and it can inhibit telomerase activity.1 Telomerase is a promising target for cancer therapy because it plays a role in immortal cell growth by elongating telomere DNA.2 Therefore, ligands that can selectively stabilize GQs have attracted in recent years great interest as a promising new class of anticancer drugs. Many G-quadruplex-ligands contain a large π-planar core and cationic functional groups; these structures facilitate π–π stacking and electrostatic interactions toward GQ’s structures.3 Porphyrinoids are ideal compounds to interact with DNA due to their peculiar characteristics.4 It has been showed that cationic porphyrins have been utilized as reporters of different sequences and conformations of single and duplex DNA.5 We explored by CD, UV, FRET and melting experiments the different effects showed by a new cationic porphyrin bearing sperminate substituents, in the presence of different conformations of GQ obtained by models of G‐rich sequences (Tel22 and TG3AG).I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
