title: 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.affiliation: Department of Chemistry, The University of Cambridge, Lensfield Road, Cambridge, CB2 1EW, UK. sb10031@cam.ac.uk.
authors.forename: Hamid R
authors.initials: HR
authors.lastname: Nasiri
authors.forename: Neil M
authors.initials: NM
authors.lastname: Bell
authors.forename: Keith I E
authors.initials: KI
authors.lastname: McLuckie
authors.forename: Jarmila
authors.initials: J
authors.lastname: Husby
authors.forename: Chris
authors.initials: C
authors.lastname: Abell
authors.forename: Stephen
authors.initials: S
authors.lastname: Neidle
authors.forename: Shankar
authors.initials: S
authors.lastname: Balasubramanian
mesh_terms: D003198:Computer Simulation; D054856:G-Quadruplexes; D006801:Humans; D008958:Models, Molecular; D011401:Promoter Regions, Genetic / Q000235:genetics; D016271:Proto-Oncogene Proteins c-myc / Q000235:genetics*
chemical_list: D016271:Proto-Oncogene Proteins c-myc