Telomerase Inhibition and Human Telomeric G-Quadruplex DNA Stabilization by a β-Carboline–Benzimidazole Derivative at Low Concentrations

Biochemistry ◽  
2017 ◽  
Vol 56 (33) ◽  
pp. 4392-4404 ◽  
Author(s):  
Kranthikumar Yadav ◽  
Penchala Narasimha Rao Meka ◽  
Sudeshna Sadhu ◽  
Sravanthi Devi Guggilapu ◽  
Jeshma Kovvuri ◽  
...  
Keyword(s):  
Benzimidazole Derivative ◽  
Telomerase Inhibition ◽  
Quadruplex Dna ◽  
Low Concentrations ◽  
G Quadruplex ◽  
Dna Stabilization

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.

Molecular recognition of parallel quadruplex [d-(TTGGGGT)]4 by mitoxantrone: binding with 1 : 4 stoichiometry leads to telomerase inhibition

RSC Advances ◽  
2016 ◽  
Vol 6 (75) ◽  
pp. 71652-71661 ◽  
Author(s):  
Tarikere Palakshan Pradeep ◽  
Sweta Tripathi ◽  
Ritu Barthwal
Keyword(s):  
Molecular Recognition ◽  
Thermal Stabilization ◽  
Cancer Drug ◽  
Telomerase Inhibition ◽  
Quadruplex Dna ◽  
Anti Cancer ◽  
G Quadruplex ◽  
Cd Studies

NMR and CD studies show that anti-cancer drug mitoxantrone (MTX) binds to parallel G-quadruplex DNA [d-(TTGGGGT)4] as stacked dimer at grooves leading to increase in thermal stabilization of DNA by ~25 °C and inhibits telomerase with IC50 = 2 μM.

scholarly journals Importance of Chiral Recognition in Designing Metal-Free Ligands for G-Quadruplex DNA

Molecules ◽  
2019 ◽  
Vol 24 (8) ◽  
pp. 1473 ◽  
Author(s):  
Dora M. Răsădean ◽  
Samuel W. O. Harrison ◽  
Isobel R. Owens ◽  
Aucéanne Miramont ◽  
Frances M. Bromley ◽  
...  
Keyword(s):  
Amino Acid ◽  
Chiral Recognition ◽  
Organic Molecules ◽  
Small Organic Molecules ◽  
Quadruplex Dna ◽  
Metal Free ◽  
G Quadruplex ◽  
Dna Stabilization

Four pairs of amino acid-functionalized naphthalenediimide enantiomers (d- and l-lysine derived NDIs) were screened toward G-quadruplex forming sequences in telomeres (h-TELO) and oncogene promoters: c-KIT1, c-KIT2, k-RAS and BCL-2. This is the first study to address the effect of point chirality toward G-quadruplex DNA stabilization using purely small organic molecules. Enantioselective behavior toward the majority of ligands was observed, particularly in the case of parallel conformations of c-KIT2 and k-RAS. Additionally, Nε-Boc-l-Lys-NDI and Nε-Boc-d-Lys-NDI discriminate between quadruplexes with parallel and hybrid topologies, which has not previously been observed with enantiomeric ligands.

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