Ontology highlight
ABSTRACT:
SUBMITTER: Zoppi V
PROVIDER: S-EPMC6348446 | biostudies-literature | 2019 Jan
REPOSITORIES: biostudies-literature
Zoppi Vittoria V Hughes Scott J SJ Maniaci Chiara C Testa Andrea A Gmaschitz Teresa T Wieshofer Corinna C Koegl Manfred M Riching Kristin M KM Daniels Danette L DL Spallarossa Andrea A Ciulli Alessio A
Journal of medicinal chemistry 20181228 2
Developing PROTACs to redirect the ubiquitination activity of E3 ligases and potently degrade a target protein within cells can be a lengthy and unpredictable process, and it remains unclear whether any combination of E3 and target might be productive for degradation. We describe a probe-quality degrader for a ligase-target pair deemed unsuitable: the von Hippel-Lindau (VHL) and BRD9, a bromodomain-containing subunit of the SWI/SNF chromatin remodeling complex BAF. VHL-based degraders could be o ...[more]