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Carbazole ligands as c-myc G-quadruplex binders

Głuszyńska, A; Juskowiak, B; Kuta-Siejkowska, M; Hoffmann, M; Haider, S; (2018) Carbazole ligands as c-myc G-quadruplex binders. International Journal of Biological Macromolecules , 114 pp. 479-490. 10.1016/j.ijbiomac.2018.03.135. Green open access

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Abstract

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.

Type: Article
Title: Carbazole ligands as c-myc G-quadruplex binders
Location: Netherlands
Open access status: An open access version is available from UCL Discovery
DOI: 10.1016/j.ijbiomac.2018.03.135
Publisher version: https://doi.org/10.1016/j.ijbiomac.2018.03.135
Language: English
Additional information: This version is the author accepted manuscript. For information on re-use, please refer to the publisher’s terms and conditions.
Keywords: Carbazole derivatives, Molecular modeling, Pu22, Spectroscopy, c-myc G-quadruplex
UCL classification: UCL
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy > Pharma and Bio Chemistry
URI: https://discovery.ucl.ac.uk/id/eprint/10047724
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