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 …
Proteolysis targeting chimeras (PROTACs) come of age: entering the third decade of targeted protein degradation
With the discovery of PROteolysis TArgeting Chimeras (PROTACs) twenty years ago,
targeted protein degradation (TPD) has changed the landscape of drug development …
targeted protein degradation (TPD) has changed the landscape of drug development …
Rational chemical design of molecular glue degraders
ES Toriki, JW Papatzimas, K Nishikawa… - ACS central …, 2023 - ACS Publications
Targeted protein degradation with molecular glue degraders has arisen as a powerful
therapeutic modality for eliminating classically undruggable disease-causing proteins …
therapeutic modality for eliminating classically undruggable disease-causing proteins …
Exploring targeted degradation strategy for oncogenic KRASG12C
KRAS is the most frequently mutated oncogene found in pancreatic, colorectal, and lung
cancers. Although it has been challenging to identify targeted therapies for cancers …
cancers. Although it has been challenging to identify targeted therapies for cancers …
Discovery of a covalent FEM1B recruiter for targeted protein degradation applications
NJ Henning, AG Manford, JN Spradlin… - Journal of the …, 2022 - ACS Publications
Proteolysis-targeting chimeras (PROTACs), heterobifunctional compounds that consist of
protein-targeting ligands linked to an E3 ligase recruiter, have arisen as a powerful …
protein-targeting ligands linked to an E3 ligase recruiter, have arisen as a powerful …
Proteolysis targeting chimera (PROTAC) in drug discovery paradigm: Recent progress and future challenges
S Zeng, W Huang, X Zheng, Z Zhang, J Wang… - European journal of …, 2021 - Elsevier
Proteolysis targeting chimera (PROTAC), hijacking protein of interest (POI) and recruiting E3
ligase for target degradation via the ubiquitin-proteasome pathway, is a novel drug …
ligase for target degradation via the ubiquitin-proteasome pathway, is a novel drug …
Selective inhibitors of SARM1 targeting an allosteric cysteine in the autoregulatory ARM domain
HC Feldman, E Merlini, C Guijas… - Proceedings of the …, 2022 - National Acad Sciences
The nicotinamide adenine dinucleotide hydrolase (NADase) sterile alpha toll/interleukin
receptor motif containing-1 (SARM1) acts as a central executioner of programmed axon …
receptor motif containing-1 (SARM1) acts as a central executioner of programmed axon …
PROTAC degraders as chemical probes for studying target biology and target validation
Small molecule degraders such as PROTACs (PROteolysis TArgeting Chimeras) have
emerged as new promising pharmacological modalities and the first PROTAC drug …
emerged as new promising pharmacological modalities and the first PROTAC drug …
DCAF11 supports targeted protein degradation by electrophilic proteolysis-targeting chimeras
X Zhang, LM Luukkonen, CL Eissler… - Journal of the …, 2021 - ACS Publications
Ligand-induced protein degradation has emerged as a compelling approach to promote the
targeted elimination of proteins from cells by directing these proteins to the ubiquitin …
targeted elimination of proteins from cells by directing these proteins to the ubiquitin …
DCAF1-based PROTACs with activity against clinically validated targets overcoming intrinsic-and acquired-degrader resistance
M Schröder, M Renatus, X Liang, F Meili… - Nature …, 2024 - nature.com
Targeted protein degradation (TPD) mediates protein level through small molecule induced
redirection of E3 ligases to ubiquitinate neo-substrates and mark them for proteasomal …
redirection of E3 ligases to ubiquitinate neo-substrates and mark them for proteasomal …