scholarly journals Kinetic Target‐Guided Synthesis of Small‐Molecule G‐Quadruplex Stabilizers

ChemistryOpen ◽  
2020 ◽  
Vol 9 (12) ◽  
pp. 1236-1250
Author(s):  
Alice Pomeislová ◽  
Lukáš Vrzal ◽  
Jaroslav Kozák ◽  
Juraj Dobiaš ◽  
Martin Hubálek ◽  
...  
Keyword(s):  
Small Molecule ◽  
G Quadruplex

scholarly journals Molecular Recognition of the Hybrid-Type G-Quadruplexes in Human Telomeres

Molecules ◽  
2019 ◽  
Vol 24 (8) ◽  
pp. 1578 ◽  
Author(s):  
Guanhui Wu ◽  
Luying Chen ◽  
Wenting Liu ◽  
Danzhou Yang
Keyword(s):  
Small Molecule ◽  
Solution Structure ◽  
Structural Information ◽  
Rational Drug Design ◽  
Hybrid Type ◽  
G4 Dna ◽  
Rational Drug ◽  
G Quadruplex ◽  
Molecule Recognition ◽  
Dna Secondary Structures

G-quadruplex (G4) DNA secondary structures formed in human telomeres have been shown to inhibit cancer-specific telomerase and alternative lengthening of telomere (ALT) pathways. Thus, human telomeric G-quadruplexes are considered attractive targets for anticancer drugs. Human telomeric G-quadruplexes are structurally polymorphic and predominantly form two hybrid-type G-quadruplexes, namely hybrid-1 and hybrid-2, under physiologically relevant solution conditions. To date, only a handful solution structures are available for drug complexes of human telomeric G-quadruplexes. In this review, we will describe two recent solution structural studies from our labs. We use NMR spectroscopy to elucidate the solution structure of a 1:1 complex between a small molecule epiberberine and the hybrid-2 telomeric G-quadruplex, and the structures of 1:1 and 4:2 complexes between a small molecule Pt-tripod and the hybrid-1 telomeric G-quadruplex. Structural information of small molecule complexes can provide important information for understanding small molecule recognition of human telomeric G-quadruplexes and for structure-based rational drug design targeting human telomeric G-quadruplexes.

Abstract 3089: A novel G-quadruplex formed in the PDGFR-β promoter that is selectively targeted by a small molecule to repress transcription

2016 ◽  
Author(s):  
Buket Onel ◽  
Prashansa Agrawal ◽  
Megan Carver ◽  
Robert Brown ◽  
Laurence Hurley ◽  
...  
Keyword(s):  
Small Molecule ◽  
G Quadruplex

Abstract 322: Selective inhibition of MYC expression by a small molecule G-quadruplex stabilizer

2016 ◽  
Author(s):  
Elena C. Leon ◽  
John K. Simmons ◽  
David Calabrese ◽  
Wendy DuBois ◽  
Kenneth Felsenstein ◽  
...  
Keyword(s):  
Small Molecule ◽  
Selective Inhibition ◽  
G Quadruplex

Abstract B40: Selective suppression of Myc transcription with a G-quadruplex stabilizing small molecule

2015 ◽  
Author(s):  
John K. Simmons ◽  
Lindsey B. Saunders ◽  
Kenneth Felsenstein ◽  
Peter Gareiss ◽  
Shuling Zhang ◽  
...  
Keyword(s):  
Small Molecule ◽  
Selective Suppression ◽  
G Quadruplex

G‐Quadruplex‐Binding Small Molecule Induces Synthetic Lethality in Breast Cancer Cells by Inhibiting c‐MYC and BCL2 Expression

ChemBioChem ◽  
2020 ◽  
Vol 21 (7) ◽  
pp. 963-970 ◽  
Author(s):  
Rakesh Paul ◽  
Tania Das ◽  
Manish Debnath ◽  
Ajay Chauhan ◽  
Jyotirmayee Dash
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Small Molecule ◽  
Breast Cancer Cells ◽  
Synthetic Lethality ◽  
G Quadruplex ◽  
Bcl2 Expression

scholarly journals Triarylpyridines: a versatile small molecule scaffold for G-quadruplex recognition

2008 ◽  
pp. 1467 ◽  
Author(s):  
Zoë A. E. Waller ◽  
Pravin S. Shirude ◽  
Raphaël Rodriguez ◽  
Shankar Balasubramanian
Keyword(s):  
Small Molecule ◽  
G Quadruplex

Metal ions modulate the conformation and stability of a G-quadruplex with or without a small-molecule ligand

Metallomics ◽  
2015 ◽  
Vol 7 (11) ◽  
pp. 1508-1514 ◽  
Author(s):  
Huiru Lu ◽  
Shenghui Li ◽  
Jun Chen ◽  
Jing Xia ◽  
Jinchao Zhang ◽  
...  
Keyword(s):  
Metal Ions ◽  
Small Molecule ◽  
G Quadruplex ◽  
Small Molecule Ligand

scholarly journals Dual Binding of an Antibody and a Small Molecule Increases the Stability of TERRA G-Quadruplex

2014 ◽  
Vol 54 (3) ◽  
pp. 910-913 ◽  
Author(s):  
Philip M. Yangyuoru ◽  
Marco Di Antonio ◽  
Chiran Ghimire ◽  
Giulia Biffi ◽  
Shankar Balasubramanian ◽  
...  
Keyword(s):  
Small Molecule ◽  
G Quadruplex ◽  
The Stability
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