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The emerging role of targeted protein degradation to treat and study cancer
MH Brodermann, EK Henderson… - The Journal of …, 2024 - Wiley Online Library
The evolution of cancer treatment has provided increasingly targeted strategies both in the
upfront and relapsed disease settings. Small‐molecule inhibitors and immunotherapy have …
upfront and relapsed disease settings. Small‐molecule inhibitors and immunotherapy have …
Degron tagging for rapid protein degradation in mice
BA Hernández-Morán, G Taylor… - Disease Models & …, 2024 - journals.biologists.com
Degron tagging allows proteins of interest to be rapidly degraded, in a reversible and
tuneable manner, in response to a chemical stimulus. This provides numerous opportunities …
tuneable manner, in response to a chemical stimulus. This provides numerous opportunities …
Discovery of CRBN-dependent WEE1 molecular glue degraders from a multicomponent combinatorial library
Small molecules promoting protein–protein interactions produce a range of therapeutic
outcomes. Molecular glue degraders exemplify this concept due to their compact drug-like …
outcomes. Molecular glue degraders exemplify this concept due to their compact drug-like …
Combination of AID2 and BromoTag expands the utility of degron-based protein knockdowns
Acute protein knockdown is a powerful approach to dissecting protein function in dynamic
cellular processes. We previously reported an improved auxin-inducible degron system …
cellular processes. We previously reported an improved auxin-inducible degron system …
Mining the CRBN Target Space Redefines Rules for Molecular Glue-induced Neosubstrate Recognition
G Petzold, P Gainza, S Annunziato, I Lamberto… - bioRxiv, 2024 - biorxiv.org
The CRL4CRBN ubiquitin ligase is leveraged by molecular glue degraders, small molecules
that reprogram ligase specificity to induce degradation of clinically relevant neosubstrate …
that reprogram ligase specificity to induce degradation of clinically relevant neosubstrate …
Degradation bottlenecks and resource competition in transiently and stably engineered mammalian cells
Degradation tags, otherwise known as degrons, are portable sequences that can be used to
alter protein stability. Here, we report that degron-tagged proteins compete for cellular …
alter protein stability. Here, we report that degron-tagged proteins compete for cellular …
Lessons from natural molecular glue degraders
S Cao - Biochemical Society Transactions, 2024 - portlandpress.com
Molecular glue (MG) degraders include plant hormones and therapeutic drugs and have
become a hot topic in drug discovery. Unlike bivalent proteolysis targeting chimeras …
become a hot topic in drug discovery. Unlike bivalent proteolysis targeting chimeras …
Systematic evolution of functional oligonucleotides for targeted protein degradation
H Su, Y Chen, X Zhao, Z Lu, T Wei, Q Liu, X Liu… - Chem, 2025 - cell.com
Targeted protein degradation (TPD) technologies leveraging the ubiquitin-proteasome
system address" undruggable" proteins but struggle with optimizing targeting warheads and …
system address" undruggable" proteins but struggle with optimizing targeting warheads and …
[HTML][HTML] GPCR-targeted PROTACs in Cancer Therapeutics
G protein-coupled receptors (GPCRs) comprise a family of heptahelical membrane proteins
that mediate intra-and inter-cellular transmembrane signaling. Defects in GPCR signaling …
that mediate intra-and inter-cellular transmembrane signaling. Defects in GPCR signaling …
High-throughput diversification of protein-ligand surfaces to discover chemical inducers of proximity
JB Shaum, EA Steen, M Muñoz i Ordoño, DV Wenge… - bioRxiv, 2024 - biorxiv.org
Chemical inducers of proximity (CIPs) stabilize biomolecular interactions, often causing a
privileged rewiring of cellular biochemistry. While rational design strategies can expedite the …
privileged rewiring of cellular biochemistry. While rational design strategies can expedite the …