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.

Authors:

HR Nasiri, NM Bell, KIE McLuckie, J Husby, C Abell, S Neidle, S Balasubramanian

Journal:

Chem Commun (Camb)

Citation info:

50(14):1704-1707

Publication date:

18th Feb 2014

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