Group-Based Optimization of Potent and Cell-Active Inhibitors of the von Hippel–Lindau (VHL) E3 Ubiquitin Ligase: Structure–Activity Relationships Leading to the Chemical Probe (2<i>S</i>,4<i>R</i>)-1-((<i>S</i>)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-<i>N</i>-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (VH298)
Pedro Soares(University of Dundee), Alessio Ciulli(University of Dundee)
Cited by 161
Related Papers
Structural basis of PROTAC cooperative recognition for selective protein degradation
|Nature Chemical Biology|2017|1.2k
Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4
|ACS Chemical Biology|2015|1k
BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design
|Nature Chemical Biology|2019|571
Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel–Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7
|Journal of Medicinal Chemistry|2018|330
Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition
|Nature Communications|2016|241