Ontology highlight
ABSTRACT:
SUBMITTER: Jung KY
PROVIDER: S-EPMC4955407 | biostudies-literature | 2015 Apr
REPOSITORIES: biostudies-literature
Jung Kwan-Young KY Wang Huabo H Teriete Peter P Yap Jeremy L JL Chen Lijia L Lanning Maryanna E ME Hu Angela A Lambert Lester J LJ Holien Toril T Sundan Anders A Cosford Nicholas D P ND Prochownik Edward V EV Fletcher Steven S
Journal of medicinal chemistry 20150330 7
The rational design of inhibitors of the bHLH-ZIP oncoprotein c-Myc is hampered by a lack of structure in its monomeric state. We describe herein the design of novel, low-molecular-weight, synthetic α-helix mimetics that recognize helical c-Myc in its transcriptionally active coiled-coil structure in association with its obligate bHLH-ZIP partner Max. These compounds perturb the heterodimer's binding to its canonical E-box DNA sequence without causing protein-protein dissociation, heralding a ne ...[more]