2JWQ
G-quadruplex recognition by quinacridines: a SAR, NMR and Biological study
Summary for 2JWQ
| Entry DOI | 10.2210/pdb2jwq/pdb |
| Descriptor | 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) |
| Functional Keywords | g-quadruplex, quinacridine, telomerase inhibitors, dna |
| Total number of polymer chains | 4 |
| Total formula weight | 9518.91 |
| Authors | Hounsou, C.,Guittat, L.,Monchaud, D.,Jourdan, M.,Saettel, N.,Mergny, J.L.,Teulade-Fichou, M. (deposition date: 2007-10-23, release date: 2008-03-25, Last modification date: 2024-05-29) |
| Primary citation | 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 Cited by 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: 17385760DOI: 10.1002/cmdc.200600286 PDB entries with the same primary citation |
| Experimental method | SOLUTION NMR |
Structure validation
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