Article (Scientific journals)
Ascididemin and meridine stabilise G-quadruplexes and inhibit telomerase in vitro
Guittat, Lionel; De Cian, Anne; Rosu, Frédéric et al.
2005In Biochimica et Biophysica Acta - General Subjects, 1724 (3), p. 375-384
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Keywords :
telomeres; telomerase inhibitor; G-quadruplex; noncovalent; DNA; mass spectrometry
Abstract :
[en] Ascididemin and Meridine are two marine compounds with pyridoacridine skeletons known to exhibit interesting antitumour activities. These molecules have been reported to behave like DNA intercalators. In this study, dialysis competition assay and mass spectrometry experiments were used to determine the affinity of ascididemin and meridine for DNA structures among duplexes, triplexes, quadruplexes and single-strands. Our data confirm that ascididemin and meridine interact with DNA but also recognize triplex and quadruplex structures. These molecules exhibit a significant preference for quadruplexes over duplexes or single-strands. Meridine is a stronger quadruplex ligand and therefore a stronger telomerase inhibitor than ascididemin (IC50= 11 and > 80 mu M, respectively in a standard TRAP assay). (c) 2005 Elsevier B.V. All rights reserved.
Research center :
CART - Centre Interfacultaire d'Analyse des Résidus en Traces - ULiège
Disciplines :
Biochemistry, biophysics & molecular biology
Chemistry
Author, co-author :
Guittat, Lionel;  Museum National d’Histoire Naturelle > INSERM UR 565, CNRS UMR 5153 > Laboratoire de Biophysique
De Cian, Anne;  Museum National d'Histoire Naturelle > INSERM UR 565, CNRS UMR 5153 > Laboratoire de Biophysique
Rosu, Frédéric ;  Université de Liège - ULiège > Département de Chimie (Sciences) > Chimie physique, spectrométrie de masse
Gabelica, Valérie ;  Université de Liège - ULiège > Département de Chimie (Sciences) > Chimie physique, spectrométrie de masse
De Pauw, Edwin  ;  Université de Liège - ULiège > Département de Chimie (Sciences) > Chimie physique, spectrométrie de masse
Delfourne, Evelyne;  Université Paul Sabatier > UMR CNRS 5068 > Laboratoire SPCMIB
Mergny, Jean-Louis;  Museum National d'Histoire Naturelle > INSERM UR 565, CNRS UMR 5153 > Laboratoire de Biophysique
Language :
English
Title :
Ascididemin and meridine stabilise G-quadruplexes and inhibit telomerase in vitro
Publication date :
2005
Journal title :
Biochimica et Biophysica Acta - General Subjects
ISSN :
0304-4165
eISSN :
1872-8006
Publisher :
Elsevier Science, Amsterdam, Netherlands
Volume :
1724
Issue :
3
Pages :
375-384
Peer reviewed :
Peer Reviewed verified by ORBi
Funders :
F.R.S.-FNRS - Fonds de la Recherche Scientifique [BE]
Commentary :
This is a postprint author version of an article published in: Biochim. Biophys. Acta (2005), 1724, 375-384.
Available on ORBi :
since 16 September 2008

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