Carbazole ligands as c-myc G-quadruplex binders
| Autor: | Marcin Hoffmann, Bernard Juskowiak, Shozeb Haider, Martyna Kuta-Siejkowska, Agata Głuszyńska |
|---|---|
| Rok vydání: | 2017 |
| Předmět: |
0301 basic medicine
Circular dichroism Molecular model Stereochemistry Triazole Carbazoles Genes myc 010402 general chemistry G-quadruplex Ligands 01 natural sciences Biochemistry 03 medical and health sciences chemistry.chemical_compound Structural Biology Imidazole Humans heterocyclic compounds Molecular Biology Chemistry Ligand Carbazole General Medicine 0104 chemical sciences G-Quadruplexes 030104 developmental biology DNA |
| Zdroj: | International journal of biological macromolecules. 114 |
| ISSN: | 1879-0003 |
| Popis: | The interactions of c-myc G-quadruplex with three carbazole derivatives were investigated by UV-Vis spectrophotometry, fluorescence, CD spectroscopy, and molecular modeling. The results showed that a combination of carbazole scaffold functionalized with ethyl, triazole and imidazole groups resulted in stabilization of the intramolecular G-quadruplex formed by the DNA sequence derived from the NHE III1 region of c-myc oncogene (Pu22). Binding to the G-quadruplex Pu22 resulted in the significant increase in fluorescence intensity of complexed ligands 1-3. All ligands were capable of interacting with G4 DNA with binding stoichiometry indicating that two ligand molecules bind to G-quadruplex with comparable affinity, which agrees with binding model of end-stacking on terminal G-tetrads. |
| Databáze: | OpenAIRE |
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