Targeting a c-MYC G-quadruplex DNA with a fragment library
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-ba...
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Veröffentlicht in: | Chemical communications (Cambridge, England) England), 2014-01, Vol.50 (14), p.1704-1707 |
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container_title | Chemical communications (Cambridge, England) |
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creator | Nasiri, Hamid R Bell, Neil M McLuckie, Keith I E Husby, Jarmila Abell, Chris Neidle, Stephen Balasubramanian, Shankar |
description | 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. |
doi_str_mv | 10.1039/c3cc48390h |
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source | MEDLINE; Royal Society Of Chemistry Journals 2008-; Alma/SFX Local Collection |
subjects | Computer Simulation G-Quadruplexes Humans Models, Molecular Promoter Regions, Genetic - genetics Proto-Oncogene Proteins c-myc - genetics |
title | Targeting a c-MYC G-quadruplex DNA with a fragment library |
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