Issue 14, 2014

Targeting a c-MYC G-quadruplex DNA with a fragment library

Abstract

We report here on the screening of a fragment library against a G-quadruplex element in the human c-MYC promoter. The ten fragment hits had significant concordance between a biophysical assay, in silico modelling and c-MYC expression inhibition, highlighting the feasibility of applying a fragment-based approach to the targeting of a quadruplex nucleic acid.

Graphical abstract: Targeting a c-MYC G-quadruplex DNA with a fragment library

Supplementary files

Article information

Article type
Communication
Submitted
01 Nov 2013
Accepted
25 Nov 2013
First published
26 Nov 2013

Chem. Commun., 2014,50, 1704-1707

Targeting a c-MYC G-quadruplex DNA with a fragment library

H. R. Nasiri, N. M. Bell, K. I. E. McLuckie, J. Husby, C. Abell, S. Neidle and S. Balasubramanian, Chem. Commun., 2014, 50, 1704 DOI: 10.1039/C3CC48390H

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