2jwq

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[[Category: telomerase inhibitor]]
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Revision as of 01:02, 31 March 2008


PDB ID 2jwq

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Sites: and
Ligands: , , ,
Resources: FirstGlance, OCA, PDBsum, RCSB
Coordinates: save as pdb, mmCIF, xml



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


Overview

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.

About this Structure

2JWQ is a Single protein structure of sequence from [1]. Full crystallographic information is available from OCA.

Reference

G-Quadruplex Recognition by Quinacridines: a SAR, NMR, and Biological Study., Hounsou C, Guittat L, Monchaud D, Jourdan M, Saettel N, Mergny JL, Teulade-Fichou MP, ChemMedChem. 2007 May;2(5):655-66. PMID:17385760

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