Ontology highlight
ABSTRACT:
SUBMITTER: Lucas X
PROVIDER: S-EPMC6109845 | biostudies-literature | 2018 Aug
REPOSITORIES: biostudies-literature
Lucas Xavier X Van Molle Inge I Ciulli Alessio A
Journal of medicinal chemistry 20180808 16
Beyond the targeting of E3 ubiquitin ligases to inhibit protein homeostasis, E3 ligase binders can be repurposed as targeted protein degraders (PROTACs or molecular glues). We sought to identify new binders of the VHL E3 ligase by biophysical fragment-based screening followed by X-ray crystallographic soaking. We identified fragments binding at the ElonginC:Cullin2 interface and a new cryptic pocket in VHL, along with other potential ligandable sites predicted computationally and found to bind s ...[more]