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Chem Commun (Camb). 2014 Feb 18;50(14):1704-7. doi: 10.1039/c3cc48390h.

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

Author information

  • 1Department of Chemistry, The University of Cambridge, Lensfield Road, Cambridge, CB2 1EW, UK. sb10031@cam.ac.uk.

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.

PMID:
24394582
DOI:
10.1039/c3cc48390h
[PubMed - indexed for MEDLINE]
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