2JWQ

G-quadruplex recognition by quinacridines: a SAR, NMR and Biological study

2JWQ の概要

• エントリーDOI: 10.2210/pdb2jwq/pdb
• 分子名称: DNA (5'-D(*DTP*DTP*DAP*DGP*DGP*DGP*DT)-3'), N,N'-(dibenzo[b,j][1,7]phenanthroline-2,10-diyldimethanediyl)dipropan-1-amine (2 entities in total)
• 機能のキーワード: g-quadruplex, quinacridine, telomerase inhibitors, dna
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 9518.91

構造登録者

Hounsou, C.,Guittat, L.,Monchaud, D.,Jourdan, M.,Saettel, N.,Mergny, J.L.,Teulade-Fichou, M. (登録日: 2007-10-23, 公開日: 2008-03-25, 最終更新日: 2024-05-29)

主引用文献

Hounsou, C.,Guittat, L.,Monchaud, D.,Jourdan, M.,Saettel, N.,Mergny, J.L.,Teulade-Fichou, M.
G-Quadruplex Recognition by Quinacridines: a SAR, NMR, and Biological Study
ChemMedChem, 2:655-666, 2007

PubMed Abstract: The synthesis of a novel group of quinacridine-based ligands (MMQs) is described along with an evaluation of their G-quadruplex binding properties. A set of biophysical assays was applied to characterize their interaction with DNA quadruplexes: FRET-melting experiments and equilibrium microdialysis were used to evaluate their quadruplex affinity and their ability to discriminate quadruplexes across a broad panel of DNA structures. All data collected support the proposed model of interaction of these compounds with G-quadruplexes, which is furthermore confirmed by a solution structure determined by 2D NMR experiments. Finally, the activity of the MMQ series against tumor cell growth is reported, and the data support the potential of quadruplex-interactive compounds for use in anticancer approaches.

PubMed: 17385760
DOI: 10.1002/cmdc.200600286

実験手法

SOLUTION NMR