Targeted protein degradation: Design considerations for PROTAC development
NL Tran, GA Leconte, FM Ferguson - Current protocols, 2022 - Wiley Online Library
Targeted protein degradation has recently gained widespread interest as both a novel
therapeutic strategy and a useful tool in biomedical research. Targeted protein degraders …
therapeutic strategy and a useful tool in biomedical research. Targeted protein degraders …
[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 …
Sweet and blind spots in E3 ligase ligand space revealed by a thermophoresis-based assay
S Maiwald, C Heim, B Hernandez Alvarez… - ACS Medicinal …, 2020 - ACS Publications
Repurposing E3 ubiquitin ligases for targeted protein degradation via customized molecular
glues or proteolysis-targeting chimeras (PROTACs) is an increasingly important therapeutic …
glues or proteolysis-targeting chimeras (PROTACs) is an increasingly important therapeutic …
Impact of target warhead and linkage vector on inducing protein degradation: comparison of bromodomain and extra-terminal (BET) degraders derived from …
KH Chan, M Zengerle, A Testa… - Journal of medicinal …, 2018 - ACS Publications
The design of proteolysis-targeting chimeras (PROTACs) is a powerful small-molecule
approach for inducing protein degradation. PROTACs conjugate a target warhead to an E3 …
approach for inducing protein degradation. PROTACs conjugate a target warhead to an E3 …
Targeted protein degradation mechanisms
Y Zhang, C Loh, J Chen, N Mainolfi - Drug Discovery Today: Technologies, 2019 - Elsevier
Targeted protein degradation mediated by small molecule degraders represents an exciting
new therapeutic opportunity to eliminate disease-causing proteins. These molecules recruit …
new therapeutic opportunity to eliminate disease-causing proteins. These molecules recruit …
Basis for a ubiquitin-like protein thioester switch toggling E1–E2 affinity
Ubiquitin-like proteins (UBLs) are conjugated by dynamic E1–E2–E3 enzyme cascades. E1
enzymes activate UBLs by catalysing UBL carboxy-terminal adenylation, forming a covalent …
enzymes activate UBLs by catalysing UBL carboxy-terminal adenylation, forming a covalent …
Exploiting the cullin E3 ligase adaptor protein SKP1 for targeted protein degradation
SH Hong, A Divakaran, A Osa, OW Huang… - ACS chemical …, 2024 - ACS Publications
Targeted protein degradation with proteolysis targeting chimeras (PROTACs) is a powerful
therapeutic modality for eliminating disease-causing proteins through targeted ubiquitination …
therapeutic modality for eliminating disease-causing proteins through targeted ubiquitination …
Molecular glues for targeted protein degradation: from serendipity to rational discovery
Targeted protein degradation is a promising area in the discovery and development of
innovative therapeutics. Molecular glues mediate proximity-induced protein degradation and …
innovative therapeutics. Molecular glues mediate proximity-induced protein degradation and …
High-throughput cellular profiling of targeted protein degradation compounds using HiBiT CRISPR cell lines
Targeted protein degradation compounds, including molecular glues or proteolysis targeting
chimeras, are an exciting new therapeutic modality in small molecule drug discovery. This …
chimeras, are an exciting new therapeutic modality in small molecule drug discovery. This …
Covalent ligand screening uncovers a RNF4 E3 ligase recruiter for targeted protein degradation applications
Targeted protein degradation has arisen as a powerful strategy for drug discovery allowing
the targeting of undruggable proteins for proteasomal degradation. This approach most …
the targeting of undruggable proteins for proteasomal degradation. This approach most …