A CD Study of a Structure-Based Selection of N-Heterocyclic Bis-Carbene Gold(I) Complexes as Potential Ligands of the G-Quadruplex-Forming Human Telomeric hTel23 Sequence
Herein, we report the structure-based selection via molecular docking of four <i>N</i>-heterocyclic bis-carbene gold(I) complexes, whose potential as ligands for the hTel23 G-quadruplex structure has been investigated using circular dichroism (CD) spectroscopy, CD melting, and polyacrylamide gel electrophoresis (PAGE). The complex containing a bis(1,2,3,4,6,7,8,9-octahydro-11<i>H</i>-11<i>λ</i><sup>3</sup>-pyridazino[1,2-a]indazol-11-yl) scaffold induces a transition from the hybrid (3 + 1) topology to a prevalent parallel G-quadruplex conformation, whereas the complex featuring a bis(2-(2-acetamidoethyl)-3<i>λ</i><sup>3</sup>-imidazo[1,5-a]pyridin-3(2<i>H</i>)-yl) moiety disrupted the original G-quadruplex structure. These results deserve particular attention in light of the recent findings on the pathological involvements of G-quadruplexes in neurodegenerative diseases.
Authors
- Giuseppe Felice Mangiatordi (ORCID: https://orcid.org/0000-0003-4042-2841)
- Luisa Ronga (ORCID: https://orcid.org/0000-0002-8485-6492)
- Michele Saviano (ORCID: https://orcid.org/0000-0001-5086-2459)
- Maria Marzano (ORCID: https://orcid.org/0000-0003-0175-9185)
- Stefano D’Errico (ORCID: https://orcid.org/0000-0002-8100-3726)
- Giorgia Oliviero (ORCID: https://orcid.org/0000-0003-0765-2127)
- Diego Tesauro (ORCID: https://orcid.org/0000-0002-1556-2562)
- Pietro Delre (ORCID: https://orcid.org/0000-0002-4523-2759)
- Gabriele Travagliante (ORCID: https://orcid.org/0000-0002-5939-4257)
- Gennaro Piccialli (ORCID: https://orcid.org/0000-0002-1313-2091)
- Filippo Prencipe (ORCID: https://orcid.org/0000-0001-6426-2761)
Institutions
- Centre National de la Recherche Scientifique (FR)
- University of Trieste (IT)
- Université de Pau et des Pays de l'Adour (FR)
- University of Catania (IT)
- Institut des Sciences Analytiques et de Physico-Chimie pour l'Environnement et les Matériaux (FR)
- Centro Interuniversitario di Ricerca sui Peptidi Bioattivi (IT)
- Institute of Crystallography (IT)
- University of Naples Federico II (IT)
Publication Details
- Journal
- Molecules
- Published
- 2024-11-19
- DOI
- https://doi.org/10.3390/molecules29225446
- Citations
- 2
- Primary Topic
- DNA and Nucleic Acid Chemistry
- Type
- article
- Field-Weighted Citation Impact
- 0.47
Funders
- Università degli Studi di Napoli Federico II