Selectivity in ligand recognition of G-quadruplex loops.
A series of disubstituted acridine ligands have been cocrystallized with a bimolecular DNA G-quadruplex. The ligands have a range of cyclic amino end groups of varying size. The crystal structures show that the diagonal loop in this quadruplex results in a large cavity for these groups, in contrast to the steric constraints imposed by propeller loops in human telomeric quadruplexes. We conclude that the nature of the loop has a significant influence on ligand selectivity for particular quadruplex folds.
Campbell
Nancy H
NH
Cancer Research UK Biomolecular Structure Group, The School of Pharmacy, University of London, 29-39 Brunswick Square, London WC1N 1AX, UK.
Patel
Manisha
M
Tofa
Amina B
AB
Ghosh
Ragina
R
Parkinson
Gary N
GN
Neidle
Stephen
S
D000166:Acridines / Q000737:chemistry; D018360:Crystallography, X-Ray; D054856:G-Quadruplexes; D008024:Ligands; D008958:Models, Molecular; D009690:Nucleic Acid Conformation; D013941:Thymine / Q000737:chemistry
D000166:Acridines; D008024:Ligands; D013941:Thymine