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 …
[HTML][HTML] Driving E3 ligase substrate specificity for targeted protein degradation: lessons from nature and the laboratory
Methods to direct the degradation of protein targets with proximity-inducing molecules that
coopt the cellular degradation machinery are advancing in leaps and bounds, and diverse …
coopt the cellular degradation machinery are advancing in leaps and bounds, and diverse …
[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 …
E3 ligases meet their match: fragment-based approaches to discover new E3 ligands and to unravel E3 biology
IN Michaelides, GW Collie - Journal of medicinal chemistry, 2023 - ACS Publications
Ubiquitination is a key post-translational modification of proteins, affecting the regulation of
multiple cellular processes. Cells are equipped with over 600 ubiquitin orchestrators, called …
multiple cellular processes. Cells are equipped with over 600 ubiquitin orchestrators, called …
[HTML][HTML] Expanding PROTACtable genome universe of E3 ligases
Proteolysis-targeting chimera (PROTAC) and other targeted protein degradation (TPD)
molecules that induce degradation by the ubiquitin-proteasome system (UPS) offer new …
molecules that induce degradation by the ubiquitin-proteasome system (UPS) offer new …
Harnessing the E3 ligase KEAP1 for targeted protein degradation
Proteolysis targeting chimeras (PROTACs) represent a new class of promising therapeutic
modalities. PROTACs hijack E3 ligases and the ubiquitin-proteasome system (UPS), leading …
modalities. PROTACs hijack E3 ligases and the ubiquitin-proteasome system (UPS), leading …
[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 …
Advancing targeted protein degradation for cancer therapy
The human proteome contains approximately 20,000 proteins, and it is estimated that more
than 600 of them are functionally important for various types of cancers, including nearly 400 …
than 600 of them are functionally important for various types of cancers, including nearly 400 …
Building ubiquitination machineries: E3 ligase multi-subunit assembly and substrate targeting by PROTACs and molecular glues
S Ramachandran, A Ciulli - Current Opinion in Structural Biology, 2021 - Elsevier
Highlights•E3 ligase machineries confer specificity to protein ubiquitination.•Multi-subunit
assembly and substrate recognition impact E3 ligase activity.•Molecular glues and …
assembly and substrate recognition impact E3 ligase activity.•Molecular glues and …
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 …