“One Ring to Bind Them All”—Part II: Identification of Promising G-Quadruplex Ligands by Screening of Cyclophane-Type Macrocycles
A collection of 26 polyammonium cyclophane-type macrocycles with a large structural diversity has been screened for G-quadruplex recognition. A two-step selection procedure based on the FRET-melting assay was carried out enabling identification of macrocycles of high affinity (ΔT1/2 up to 30°C) an...
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| Format: | Article |
| Language: | English |
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Wiley
2010-01-01
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| Series: | Journal of Nucleic Acids |
| Online Access: | http://dx.doi.org/10.4061/2010/460561 |
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| author | Anton Granzhan David Monchaud Nicolas Saettel Aurore Guédin Jean-Louis Mergny Marie-Paule Teulade-Fichou |
| author_facet | Anton Granzhan David Monchaud Nicolas Saettel Aurore Guédin Jean-Louis Mergny Marie-Paule Teulade-Fichou |
| author_sort | Anton Granzhan |
| collection | DOAJ |
| description | A collection of 26 polyammonium cyclophane-type macrocycles with a large structural diversity has been screened for G-quadruplex recognition. A two-step selection procedure based on the FRET-melting assay was carried out enabling identification of macrocycles of high affinity (ΔT1/2 up to 30°C) and high selectivity for the human telomeric G-quadruplex. The four selected hits possess sophisticated architectures, more particularly the presence of a pendant side-arm as well as the existence of a particular topological arrangement appear to be strong determinants of quadruplex binding. These compounds are thus likely to create multiple contacts with the target that may be at the origin of their high selectivity, thereby suggesting that this class of macrocycles offers unique advantages for targeting G-quadruplex-DNA. |
| format | Article |
| id | doaj-art-8e5956d4aef54273a33fcbc5aeea05ee |
| institution | Kabale University |
| issn | 2090-021X |
| language | English |
| publishDate | 2010-01-01 |
| publisher | Wiley |
| record_format | Article |
| series | Journal of Nucleic Acids |
| spelling | doaj-art-8e5956d4aef54273a33fcbc5aeea05ee2025-02-03T06:01:39ZengWileyJournal of Nucleic Acids2090-021X2010-01-01201010.4061/2010/460561460561“One Ring to Bind Them All”—Part II: Identification of Promising G-Quadruplex Ligands by Screening of Cyclophane-Type MacrocyclesAnton Granzhan0David Monchaud1Nicolas Saettel2Aurore Guédin3Jean-Louis Mergny4Marie-Paule Teulade-Fichou5Section Recherche, Institut Curie, CNRS UMR176, Centre Universitaire Paris XI, Bat. 110, 91405 Orsay, FranceSection Recherche, Institut Curie, CNRS UMR176, Centre Universitaire Paris XI, Bat. 110, 91405 Orsay, FranceSection Recherche, Institut Curie, CNRS UMR176, Centre Universitaire Paris XI, Bat. 110, 91405 Orsay, FranceINSERM, U565, Acides Nucléiques : Dynamique, Ciblage et Fonctions Biologiques & CNRS, UMR5153, Laboratoire des Régulations et Dynamique du Génome, Muséum National d'histoire Naturelle USM 503, 43, Rue Cuvier, 75005 Paris, FranceINSERM U869, Institut Européen de Chimie et Biologie, Université de Bordeaux, 33607 Pessac cedex, FranceSection Recherche, Institut Curie, CNRS UMR176, Centre Universitaire Paris XI, Bat. 110, 91405 Orsay, FranceA collection of 26 polyammonium cyclophane-type macrocycles with a large structural diversity has been screened for G-quadruplex recognition. A two-step selection procedure based on the FRET-melting assay was carried out enabling identification of macrocycles of high affinity (ΔT1/2 up to 30°C) and high selectivity for the human telomeric G-quadruplex. The four selected hits possess sophisticated architectures, more particularly the presence of a pendant side-arm as well as the existence of a particular topological arrangement appear to be strong determinants of quadruplex binding. These compounds are thus likely to create multiple contacts with the target that may be at the origin of their high selectivity, thereby suggesting that this class of macrocycles offers unique advantages for targeting G-quadruplex-DNA.http://dx.doi.org/10.4061/2010/460561 |
| spellingShingle | Anton Granzhan David Monchaud Nicolas Saettel Aurore Guédin Jean-Louis Mergny Marie-Paule Teulade-Fichou “One Ring to Bind Them All”—Part II: Identification of Promising G-Quadruplex Ligands by Screening of Cyclophane-Type Macrocycles Journal of Nucleic Acids |
| title | “One Ring to Bind Them All”—Part II: Identification of Promising G-Quadruplex Ligands by Screening of Cyclophane-Type Macrocycles |
| title_full | “One Ring to Bind Them All”—Part II: Identification of Promising G-Quadruplex Ligands by Screening of Cyclophane-Type Macrocycles |
| title_fullStr | “One Ring to Bind Them All”—Part II: Identification of Promising G-Quadruplex Ligands by Screening of Cyclophane-Type Macrocycles |
| title_full_unstemmed | “One Ring to Bind Them All”—Part II: Identification of Promising G-Quadruplex Ligands by Screening of Cyclophane-Type Macrocycles |
| title_short | “One Ring to Bind Them All”—Part II: Identification of Promising G-Quadruplex Ligands by Screening of Cyclophane-Type Macrocycles |
| title_sort | one ring to bind them all part ii identification of promising g quadruplex ligands by screening of cyclophane type macrocycles |
| url | http://dx.doi.org/10.4061/2010/460561 |
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