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 …
Target and tissue selectivity of PROTAC degraders
RG Guenette, SW Yang, J Min, B Pei… - Chemical Society …, 2022 - pubs.rsc.org
Targeted protein degradation (TPD) strategies have revolutionized how scientists tackle
challenging protein targets deemed undruggable with traditional small molecule inhibitors …
challenging protein targets deemed undruggable with traditional small molecule inhibitors …
Chasing molecular glue degraders: screening approaches
A Domostegui, L Nieto-Barrado… - Chemical Society …, 2022 - pubs.rsc.org
Protein–protein interactions (PPIs) govern all biological processes. Some small molecules
modulate PPIs through induced protein proximity. In particular, molecular glue degraders …
modulate PPIs through induced protein proximity. In particular, molecular glue degraders …
Rational discovery of molecular glue degraders via scalable chemical profiling
C Mayor-Ruiz, S Bauer, M Brand, Z Kozicka… - Nature chemical …, 2020 - nature.com
Targeted protein degradation is a new therapeutic modality based on drugs that destabilize
proteins by inducing their proximity to E3 ubiquitin ligases. Of particular interest are …
proteins by inducing their proximity to E3 ubiquitin ligases. Of particular interest are …
Cullin-RING ubiquitin ligase regulatory circuits: a quarter century beyond the F-box hypothesis
JW Harper, BA Schulman - Annual review of biochemistry, 2021 - annualreviews.org
Cullin-RING ubiquitin ligases (CRLs) are dynamic modular platforms that regulate myriad
biological processes through target-specific ubiquitylation. Our knowledge of this system …
biological processes through target-specific ubiquitylation. Our knowledge of this system …
Clinical significance of FBXW7 loss of function in human cancers
J Fan, M Bellon, M Ju, L Zhao, M Wei, L Fu, C Nicot - Molecular cancer, 2022 - Springer
Abstract FBXW7 (F-Box and WD Repeat Domain Containing 7)(also referred to as FBW7 or
hCDC4) is a component of the Skp1-Cdc53/Cullin-F-box-protein complex (SCF/β-TrCP). As …
hCDC4) is a component of the Skp1-Cdc53/Cullin-F-box-protein complex (SCF/β-TrCP). As …
Ubiquitin ligation to F-box protein targets by SCF–RBR E3–E3 super-assembly
D Horn-Ghetko, DT Krist, JR Prabu, K Baek… - Nature, 2021 - nature.com
E3 ligases are typically classified by hallmark domains such as RING and RBR, which are
thought to specify unique catalytic mechanisms of ubiquitin transfer to recruited substrates …
thought to specify unique catalytic mechanisms of ubiquitin transfer to recruited substrates …
E3-specific degrader discovery by dynamic tracing of substrate receptor abundance
Targeted protein degradation (TPD) is a new pharmacology based on small-molecule
degraders that induce proximity between a protein of interest (POI) and an E3 ubiquitin …
degraders that induce proximity between a protein of interest (POI) and an E3 ubiquitin …
Systemwide disassembly and assembly of SCF ubiquitin ligase complexes
K Baek, DC Scott, LT Henneberg, MT King, M Mann… - Cell, 2023 - cell.com
Cells respond to environmental cues by remodeling their inventories of multiprotein
complexes. Cellular repertoires of SCF (SKP1-CUL1-F box protein) ubiquitin ligase …
complexes. Cellular repertoires of SCF (SKP1-CUL1-F box protein) ubiquitin ligase …
Proteome-scale discovery of protein degradation and stabilization effectors
J Poirson, H Cho, A Dhillon, S Haider, AZ Imrit… - Nature, 2024 - nature.com
Targeted protein degradation and stabilization are promising therapeutic modalities
because of their potency, versatility and their potential to expand the druggable target …
because of their potency, versatility and their potential to expand the druggable target …