Proximity-based modalities for biology and medicine
Molecular proximity orchestrates biological function, and blocking existing proximities is an
established therapeutic strategy. By contrast, strengthening or creating neoproximity with …
established therapeutic strategy. By contrast, strengthening or creating neoproximity with …
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 …
Chemical specification of E3 ubiquitin ligase engagement by cysteine-reactive chemistry
Targeted protein degradation relies on small molecules that induce new protein–protein
interactions between targets and the cellular protein degradation machinery. Most of these …
interactions between targets and the cellular protein degradation machinery. Most of these …
Co-opting the E3 ligase KLHDC2 for targeted protein degradation by small molecules
CM Hickey, KM Digianantonio… - Nature Structural & …, 2024 - nature.com
Targeted protein degradation (TPD) by PROTAC (proteolysis-targeting chimera) and
molecular glue small molecules is an emerging therapeutic strategy. To expand the roster of …
molecular glue small molecules is an emerging therapeutic strategy. To expand the roster of …
Unlocking DCAFs To Catalyze Degrader Development: An Arena for Innovative Approaches
Chemically induced proximity-based targeted protein degradation (TPD) has become a
prominent paradigm in drug discovery. With the clinical benefit demonstrated by certain …
prominent paradigm in drug discovery. With the clinical benefit demonstrated by certain …
[HTML][HTML] Exploration of the tunability of BRD4 degradation by DCAF16 trans-labelling covalent glues
Small molecules that can induce protein degradation by inducing proximity between a
desired target and an E3 ligase have the potential to greatly expand the number of proteins …
desired target and an E3 ligase have the potential to greatly expand the number of proteins …
DCAF16-Based Covalent Handle for the Rational Design of Monovalent Degraders
Targeted protein degradation with monovalent molecular glue degraders is a powerful
therapeutic modality for eliminating disease causing proteins. However, rational design of …
therapeutic modality for eliminating disease causing proteins. However, rational design of …
Optimization of Potent Ligands for the E3 Ligase DCAF15 and Evaluation of Their Use in Heterobifunctional Degraders
SCC Lucas, A Ahmed, SN Ashraf… - Journal of Medicinal …, 2024 - ACS Publications
Unlocking novel E3 ligases for use in heterobifunctional PROTAC degraders is of high
importance to the pharmaceutical industry. Over-reliance on the current suite of ligands used …
importance to the pharmaceutical industry. Over-reliance on the current suite of ligands used …
[HTML][HTML] Chemoproteomic Covalent Ligand Discovery as the PROTAC-gonist: The Future of Targeted Degradation Medicines
K Shishikura, ML Matthews - 2024 - ACS Publications
Chemoproteomic Covalent Ligand Discovery as the PROTAC-gonist: The Future of Targeted
Degradation Medicines | ACS Central Science Recently Viewedclose modal Pair your accounts …
Degradation Medicines | ACS Central Science Recently Viewedclose modal Pair your accounts …
Molecular glues and induced proximity: An evolution of tools and discovery
SA Robinson, SM Banik - Cell Chemical Biology, 2024 - cell.com
Small molecule molecular glues can nucleate protein complexes and rewire interactomes.
Molecular glues are widely used as probes for understanding functional proximity at a …
Molecular glues are widely used as probes for understanding functional proximity at a …