Novel ruthenium(ii) polypyridyl complexes as G-quadruplex stabilisers and telomerase inhibitors

2014 ◽  
Vol 43 (21) ◽  
pp. 7811 ◽  
Author(s):  
Guoliang Liao ◽  
Xiang Chen ◽  
Jingheng Wu ◽  
Chen Qian ◽  
Hanqiang Wang ◽  
...  
Keyword(s):  
Polypyridyl Complexes ◽  
Telomerase Inhibitors ◽  
G Quadruplex

scholarly journals Design and study of telomerase inhibitors based on G-quadruplex ligands

2013 ◽  
Vol 29 (3) ◽  
pp. 169-176 ◽  
Author(s):  
V. V. Negrutska ◽  
L. V. Dubey ◽  
M. M. Ilchenko ◽  
I. Ya. Dubey
Keyword(s):  
Telomerase Inhibitors ◽  
G Quadruplex

scholarly journals Selective Binding of Distamycin A Derivative to G-Quadruplex Structure [d(TGGGGT)]4

2010 ◽  
Vol 2010 ◽  
pp. 1-7 ◽  
Author(s):  
Bruno Pagano ◽  
Iolanda Fotticchia ◽  
Stefano De Tito ◽  
Carlo A. Mattia ◽  
Luciano Mayol ◽  
...  
Keyword(s):  
Small Molecules ◽  
Titration Calorimetry ◽  
Distamycin A ◽  
Structural Modifications ◽  
Telomerase Inhibitors ◽  
G Quadruplex ◽  
Nmr Techniques ◽  
Eukaryotic Organisms ◽  
New Anticancer Drugs ◽  
Binding Behaviour

Guanine-rich nucleic acid sequences can adopt G-quadruplex structures stabilized by layers of four Hoogsteen-paired guanine residues. Quadruplex-prone sequences are found in many regions of human genome and in the telomeres of all eukaryotic organisms. Since small molecules that target G-quadruplexes have been found to be effective telomerase inhibitors, the identification of new specific ligands for G-quadruplexes is emerging as a promising approach to develop new anticancer drugs. Distamycin A is known to bind to AT-rich sequences of duplex DNA, but it has recently been shown to interact also with G-quadruplexes. Here, isothermal titration calorimetry (ITC) and NMR techniques have been employed to characterize the interaction between a dicationic derivative of distamycin A (compound1) and the [d(TGGGGT)]4quadruplex. Additionally, to compare the binding behaviour of netropsin and compound1to the same target, a calometric study of the interaction between netropsin and [d(TGGGGT)]4has been performed. Experiments show that netropsin and compound1are able to bind to [d(TGGGGT)]4with good affinity and comparable thermodynamic profiles. In both cases the interactions are entropically driven processes with a small favourable enthalpic contribution. Interestingly, the structural modifications of compound1decrease the affinity of the ligand toward the duplex, enhancing the selectivity.

New dimeric carbazole–benzimidazole mixed ligands for the stabilization of human telomeric G-quadruplex DNA and as telomerase inhibitors. A remarkable influence of the spacer

2015 ◽  
Vol 13 (30) ◽  
pp. 8335-8348 ◽  
Author(s):  
Basudeb Maji ◽  
Krishan Kumar ◽  
K. Muniyappa ◽  
Santanu Bhattacharya
Keyword(s):  
Dna Binding ◽  
Inhibition Activity ◽  
Telomerase Inhibition ◽  
Quadruplex Dna ◽  
Telomerase Inhibitors ◽  
Mixed Ligands ◽  
G Quadruplex

G-quadruplex DNA binding dimeric ligands and their telomerase inhibition activity are reported.

Ruthenium(ii) polypyridyl complexes as dual inhibitors of telomerase and topoisomerase

2015 ◽  
Vol 44 (34) ◽  
pp. 15145-15156 ◽  
Author(s):  
Guoliang Liao ◽  
Xiang Chen ◽  
Jingheng Wu ◽  
Chen Qian ◽  
Yi Wang ◽  
...  
Keyword(s):  
Topoisomerase I ◽  
Polypyridyl Complexes ◽  
Quadruplex Structure ◽  
G Quadruplex ◽  
Dual Inhibitors

Three ruthenium(ii) polypyridyl complexes, [Ru(bpy)2(icip)]2+ (1), [Ru(bpy)2(pdppz)]2+ (2), and [Ru(bpy)2(tactp)]2+ (3), were selected to inhibit telomerase by inducing and stabilising the G-quadruplex structure, and behave as topoisomerase I/II poisons at the same time.

scholarly journals The Thermodynamic Effects of Ligand Structure on the Molecular Recognition of Mono- and Biruthenium Polypyridyl Complexes with G-Quadruplex DNA

2017 ◽  
Vol 2017 (33) ◽  
pp. 3953-3960 ◽  
Author(s):  
Clinton G. Mikek ◽  
Venkata R. Machha ◽  
Jake C. White ◽  
Logan R. Martin ◽  
Savannah J. West ◽  
...  
Keyword(s):  
Molecular Recognition ◽  
Polypyridyl Complexes ◽  
Quadruplex Dna ◽  
Ligand Structure ◽  
G Quadruplex ◽  
Thermodynamic Effects
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