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.
journal_name
ChemMedChemjournal_title
ChemMedChemauthors
Hounsou C,Guittat L,Monchaud D,Jourdan M,Saettel N,Mergny JL,Teulade-Fichou MPdoi
10.1002/cmdc.200600286subject
Has Abstractpub_date
2007-05-01 00:00:00pages
655-66issue
5eissn
1860-7179issn
1860-7187journal_volume
2pub_type
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