[HTML][HTML] Discovery of small molecule ligands for the von Hippel-Lindau (VHL) E3 ligase and their use as inhibitors and PROTAC degraders
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 …
proteasome system that recruits substrates such as the hypoxia inducible factor for …
E3 ligase ligand chemistries: from building blocks to protein degraders
In recent years, proteolysis-targeting chimeras (PROTACs), capable of achieving targeted
protein degradation, have proven their great therapeutic potential and usefulness as …
protein degradation, have proven their great therapeutic potential and usefulness as …
[HTML][HTML] Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation
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 ubiquitination of proteins, targeting them for proteasomal degradation. E3 ligases are …
[HTML][HTML] Cereblon versus VHL: Hijacking E3 ligases against each other using PROTACs
Abstract The von Hippel-Lindau (VHL) and cereblon (CRBN) proteins are substrate
recognition subunits of two ubiquitously expressed and biologically important Cullin RING …
recognition subunits of two ubiquitously expressed and biologically important Cullin RING …
[HTML][HTML] Discovery of E3 ligase ligands for target protein degradation
Target protein degradation has emerged as a promising strategy for the discovery of novel
therapeutics during the last decade. Proteolysis-targeting chimera (PROTAC) harnesses a …
therapeutics during the last decade. Proteolysis-targeting chimera (PROTAC) harnesses a …
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 (2S,4R …
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 ligase, which targets hydroxylated α subunit of hypoxia inducible factors (HIFs) …
Ligandability of E3 ligases for targeted protein degradation applications
Targeted protein degradation (TPD) using proteolysis targeting chimeras (PROTACs) and
molecular glue degraders has arisen as a powerful therapeutic modality for eliminating …
molecular glue degraders has arisen as a powerful therapeutic modality for eliminating …
Fragment-based covalent ligand screening enables rapid discovery of inhibitors for the RBR E3 ubiquitin ligase HOIP
H Johansson, YC Isabella Tsai, K Fantom… - Journal of the …, 2019 - ACS Publications
Modification of proteins with polyubiquitin chains is a key regulatory mechanism to control
cellular behavior and alterations in the ubiquitin system are linked to many diseases. Linear …
cellular behavior and alterations in the ubiquitin system are linked to many diseases. Linear …
[HTML][HTML] Expanding the landscape of E3 ligases for targeted protein degradation
Targeted protein degradation (TPD) is a rapidly developing field in chemical biology and
drug discovery. Various TPD modalities have emerged, with proteolysis-targeting chimeras …
drug discovery. Various TPD modalities have emerged, with proteolysis-targeting chimeras …
Targeting the von Hippel–Lindau E3 ubiquitin ligase using small molecules to disrupt the VHL/HIF-1α interaction
DL Buckley, I Van Molle, PC Gareiss… - Journal of the …, 2012 - ACS Publications
E3 ubiquitin ligases, which bind protein targets, leading to their ubiquitination and
subsequent degradation, are attractive drug targets due to their exquisite substrate …
subsequent degradation, are attractive drug targets due to their exquisite substrate …