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 …
Extrapolating Lessons from Targeted Protein Degradation to Other Proximity-Inducing Drugs
GE Winter - ACS Chemical Biology, 2024 - ACS Publications
Targeted protein degradation (TPD) is an emerging pharmacologic strategy. It relies on
small-molecule “degraders” that induce proximity of a component of an E3 ubiquitin ligase …
small-molecule “degraders” that induce proximity of a component of an E3 ubiquitin ligase …
DCAF1-based PROTACs with activity against clinically validated targets overcoming intrinsic-and acquired-degrader resistance
M Schröder, M Renatus, X Liang, F Meili… - Nature …, 2024 - nature.com
Targeted protein degradation (TPD) mediates protein level through small molecule induced
redirection of E3 ligases to ubiquitinate neo-substrates and mark them for proteasomal …
redirection of E3 ligases to ubiquitinate neo-substrates and mark them for proteasomal …
E3-specific degrader discovery by dynamic tracing of substrate receptor abundance
Targeted protein degradation (TPD) is a new pharmacology based on small-molecule
degraders that induce proximity between a protein of interest (POI) and an E3 ubiquitin …
degraders that induce proximity between a protein of interest (POI) and an E3 ubiquitin …
Targeted protein degradation via intramolecular bivalent glues
O Hsia, M Hinterndorfer, AD Cowan, K Iso, T Ishida… - bioRxiv, 2023 - biorxiv.org
Targeted protein degradation is a drug modality represented by compounds that recruit a
target to an E3 ubiquitin ligase to promote target ubiquitination and proteasomal …
target to an E3 ubiquitin ligase to promote target ubiquitination and proteasomal …
Plasticity of the Cullin-RING ligase repertoire shapes sensitivity to ligand-induced protein degradation
Inducing protein degradation via small molecules is a transformative therapeutic paradigm.
Although structural requirements of target degradation are emerging, mechanisms …
Although structural requirements of target degradation are emerging, mechanisms …
Molecular glues: the adhesive connecting targeted protein degradation to the clinic
Targeted protein degradation is a rapidly exploding drug discovery strategy that uses small
molecules to recruit disease-causing proteins for rapid destruction mainly via the ubiquitin …
molecules to recruit disease-causing proteins for rapid destruction mainly via the ubiquitin …
Reinstating targeted protein degradation with DCAF1 PROTACs in CRBN PROTAC resistant settings
M Schröder, M Renatus, X Liang, F Meili, T Zoller… - BioRxiv, 2023 - biorxiv.org
Targeted protein degradation (TPD) of neo-substrates with proteolysis targeting chimeras
(PROTACs) or molecular glues has emerged as a key modality in exploring new biology as …
(PROTACs) or molecular glues has emerged as a key modality in exploring new biology as …
Critical assessment of targeted protein degradation as a research tool and pharmacological modality
Small molecules continue to dominate drug discovery because of their ease of use, lower
cost of manufacturing, and access to intracellular targets. However, despite these …
cost of manufacturing, and access to intracellular targets. However, despite these …
Profiling the landscape of drug resistance mutations in neosubstrates to molecular glue degraders
Targeted protein degradation (TPD) holds immense promise for drug discovery, but
mechanisms of acquired resistance to degraders remain to be fully identified. Here, we used …
mechanisms of acquired resistance to degraders remain to be fully identified. Here, we used …