NMR based model of human telomeric repeat G-quadruplex in complex with 2,4,6-triarylpyridine family ligand
| Autor: | Jean-Louis Mergny, Abdelaziz Kerkour, Gilmar F. Salgado |
|---|---|
| Rok vydání: | 2017 |
| Předmět: |
0301 basic medicine
Telomerase Magnetic Resonance Spectroscopy Pyridines Stereochemistry Biophysics Drug design Antineoplastic Agents Biology Ligands G-quadruplex Biochemistry Genome Structure-Activity Relationship 03 medical and health sciences chemistry.chemical_compound Humans heterocyclic compounds Molecular Biology Sequence (medicine) Genetics Binding Sites Guanosine Chromosome DNA Telomere G-Quadruplexes Molecular Docking Simulation 030104 developmental biology chemistry Drug Design |
| Zdroj: | Biochimica et Biophysica Acta (BBA) - General Subjects. 1861:1293-1302 |
| ISSN: | 0304-4165 |
| Popis: | G-quadruplexes (G4) are one of the several different forms of non-canonical DNA structures that can occur in our genome. Their existence is thought to be implicated in important biological functions such as positive and negative transcription regulation or telomeric extension. The human telomeric sequence G4 formed by repetitive nucleotide sequences (T2AG3) at each chromosome end is an important example of intramolecular G4. Knowing the atomic details for different families of ligands targeting G-quadruplex structures hypothetically found in the telomeric repeat it is an important step for rational drug design. Especially if the aim is to prevent or interfere with telomerase extending the 3′ end of telomeres. In this study, we report the structure of the complex formed between the telomeric repeat sequence (d[AG 3 (T 2 AG 3 ) 3 ]) intramolecular G-quadruplex and the 2,4,6-Triarylpyridine compound. This article is part of a Special Issue entitled "G-quadruplex" Guest Editor: Dr. Concetta Giancola and Dr. Daniela Montesarchio. |
| Databáze: | OpenAIRE |
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