[HTML][HTML] Targeted protein degradation via intramolecular bivalent glues
O Hsia, M Hinterndorfer, AD Cowan, K Iso, T Ishida… - Nature, 2024 - nature.com
Targeted protein degradation is a pharmacological modality that is based on the induced
proximity of an E3 ubiquitin ligase and a target protein to promote target ubiquitination and …
proximity of an E3 ubiquitin ligase and a target protein to promote target ubiquitination and …
[HTML][HTML] Template-assisted covalent modification of DCAF16 underlies activity of BRD4 molecular glue degraders
Small molecules that induce protein-protein interactions to exert proximity-driven
pharmacology such as targeted protein degradation are a powerful class of therapeutics 1 …
pharmacology such as targeted protein degradation are a powerful class of therapeutics 1 …
Plasticity in binding confers selectivity in ligand-induced protein degradation
Heterobifunctional small-molecule degraders that induce protein degradation through ligase-
mediated ubiquitination have shown considerable promise as a new pharmacological …
mediated ubiquitination have shown considerable promise as a new pharmacological …
DCAF16-Based Covalent Handle for the Rational Design of Monovalent Degraders
M Lim, TD Cong, LM Orr, ES Toriki, AC Kile… - ACS Central …, 2024 - ACS Publications
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 …
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 …
[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 …
[HTML][HTML] Discovery of a DCAF11-dependent cyanoacrylamide-containing covalent degrader of BET-proteins
Targeted protein degradation is mediated by small molecules that induce or stabilize protein–
protein interactions between targets and the ubiquitin–proteasome machinery. Currently …
protein interactions between targets and the ubiquitin–proteasome machinery. Currently …
Structural basis of PROTAC cooperative recognition for selective protein degradation
Inducing macromolecular interactions with small molecules to activate cellular signaling is a
challenging goal. PROTACs (proteolysis-targeting chimeras) are bifunctional molecules that …
challenging goal. PROTACs (proteolysis-targeting chimeras) are bifunctional molecules that …
Cellular resistance mechanisms to targeted protein degradation converge toward impairment of the engaged ubiquitin transfer pathway
P Ottis, C Palladino, P Thienger, A Britschgi… - ACS chemical …, 2019 - ACS Publications
Proteolysis targeting chimeras are bifunctional small molecules capable of recruiting a target
protein of interest to an E3 ubiquitin ligase that facilitates target ubiquitination followed by …
protein of interest to an E3 ubiquitin ligase that facilitates target ubiquitination followed by …
[HTML][HTML] Targeted degradation via direct 26S proteasome recruitment
C Bashore, S Prakash, MC Johnson… - Nature Chemical …, 2023 - nature.com
Engineered destruction of target proteins by recruitment to the cell's degradation machinery
has emerged as a promising strategy in drug discovery. The majority of molecules that …
has emerged as a promising strategy in drug discovery. The majority of molecules that …