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 …
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 the ligand spaces for E3 ligases for the design of protein degraders
Targeted protein degradation (TPD) has recently emerged as an exciting new drug modality.
However, the strategy of developing small molecule-based protein degraders has evolved …
However, the strategy of developing small molecule-based protein degraders has evolved …
[HTML][HTML] Electrophilic Screening Platforms for Identifying Novel Covalent Ligands for E3 Ligases
S Zheng, CM Crews - Biochemistry, 2021 - ACS Publications
Proteolysis targeting chimeras (PROTACs) are hetero-bifunctional small molecules
comprised of an E3 ligase recruiting molecule and the ligand for a protein of interest (POI) …
comprised of an E3 ligase recruiting molecule and the ligand for a protein of interest (POI) …
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 …
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 …
High throughput E3 ligase degron binding assays for novel PROTAC ligand discovery
RG Guenette, PR Potts - Methods in Enzymology, 2023 - Elsevier
The discovery of new small molecule ligands for E3 ligases will enable the creation of novel
proteolysis targeting chimeras (PROTACs) and molecular glues to tackle traditionally …
proteolysis targeting chimeras (PROTACs) and molecular glues to tackle traditionally …
E3 ligase ligands for PROTACs: how they were found and how to discover new ones
T Ishida, A Ciulli - … Advancing the Science of Drug Discovery, 2021 - journals.sagepub.com
Bifunctional degrader molecules, also called proteolysis-targeting chimeras (PROTACs), are
a new modality of chemical tools and potential therapeutics to understand and treat human …
a new modality of chemical tools and potential therapeutics to understand and treat human …
Efficient, multi-hundred-gram scale access to E3 ubiquitin ligase ligands for degrader development
MS Cooper, MC Norley, S Armitage… - Organic & …, 2023 - pubs.rsc.org
Small molecule heterobifunctional degraders (commonly also known as PROTACs) offer
tremendous potential to deliver new therapeutics in areas of unmet medical need. To deliver …
tremendous potential to deliver new therapeutics in areas of unmet medical need. To deliver …
Driving E3 ligase substrate specificity for targeted protein degradation: lessons from nature and the laboratory
AD Cowan, A Ciulli - Annual Review of Biochemistry, 2022 - annualreviews.org
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 …