Hydroxylation and fluorination of proline alters the pyrrolidine ring pucker and the trans: cis
amide bond ratio in a stereochemistry-dependent fashion, affecting molecular recognition of …

E3 ubiquitin ligases are attractive targets in the ubiquitin–proteasome system, however, the
development of small-molecule ligands has been rewarded with limited success. The von …

The von Hippel–Lindau tumor suppressor protein is the substrate binding subunit of the VHL
E3 ubiquitin ligase, which targets hydroxylated α subunit of hypoxia inducible factors (HIFs) …

E3 ubiquitin ligases are key enzymes within the ubiquitin proteasome system which catalyze
the ubiquitination of proteins, targeting them for proteasomal degradation. E3 ligases are …

The von Hippel-Lindau (VHL) Cullin RING E3 ligase is an essential enzyme in the ubiquitin-
proteasome system that recruits substrates such as the hypoxia inducible factor for …

Targeted protein degradation is an emerging strategy for drug discovery that employs small
molecules to catalyze the ubiquitination of target proteins, ultimately causing their …

E3 ubiquitin ligases, such as the therapeutically relevant VHL, are challenging targets for
traditional medicinal chemistry, as their modulation requires targeting protein-protein …

Herein, we describe a systematic SAR‐and SPR‐investigation of the peptidomimetic
hydroxy‐proline based VHL‐ligand VH032, from which most to‐date published VHL …

Targeted protein degradation relies on small molecules that induce new protein–protein
interactions between targets and the cellular protein degradation machinery. Most of these …

Abstract The von Hippel-Lindau (VHL) and cereblon (CRBN) proteins are substrate
recognition subunits of two ubiquitously expressed and biologically important Cullin RING …