E3 ligase ligand chemistries: from building blocks to protein degraders

I Sosič, A Bricelj, C Steinebach - Chemical Society Reviews, 2022 - pubs.rsc.org
In recent years, proteolysis-targeting chimeras (PROTACs), capable of achieving targeted
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

MJ Bond, CM Crews - RSC chemical biology, 2021 - pubs.rsc.org
With the discovery of PROteolysis TArgeting Chimeras (PROTACs) twenty years ago,
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 …

Exploring targeted degradation strategy for oncogenic KRASG12C

M Zeng, Y Xiong, N Safaee, RP Nowak… - Cell chemical …, 2020 - cell.com
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 …

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 …

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 …

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 …

PROTAC degraders as chemical probes for studying target biology and target validation

V Němec, MP Schwalm, S Müller… - Chemical Society Reviews, 2022 - pubs.rsc.org
Small molecule degraders such as PROTACs (PROteolysis TArgeting Chimeras) have
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 …

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 …