Issue 29, 2020

Dual-binding conjugates of diaromatic guanidines and porphyrins for recognition of G-quadruplexes

Abstract

The first conceptualised class of dual-binding guanine quadruplex binders has been designed, synthesised and biophysically studied. These compounds combine diaromatic guanidinium systems and neutral tetra-phenylporphyrins (classical binding moiety for guanine quadruplexes) by means of a semi-rigid linker. An extensive screening of a variety of guanine quadruplex structures and double stranded DNA via UV-vis, FRET and CD experiments revealed the preference of the conjugates towards guanine quadruplexes. Additionally, docking studies indicate the potential dual mode of binding.

Graphical abstract: Dual-binding conjugates of diaromatic guanidines and porphyrins for recognition of G-quadruplexes

Supplementary files

Article information

Article type
Paper
Submitted
19 Jun 2020
Accepted
01 Jul 2020
First published
01 Jul 2020

Org. Biomol. Chem., 2020,18, 5617-5624

Dual-binding conjugates of diaromatic guanidines and porphyrins for recognition of G-quadruplexes

J. Grover, C. Trujillo, M. Saad, G. Emandi, N. Stipaničev, S. S. R. Bernhard, A. Guédin, J. Mergny, M. O. Senge and I. Rozas, Org. Biomol. Chem., 2020, 18, 5617 DOI: 10.1039/D0OB01264E

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