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 …

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 …

Discovery of CRBN-dependent WEE1 molecular glue degraders from a multicomponent combinatorial library

H Razumkov, Z Jiang, K Baek, I You… - Journal of the …, 2024 - ACS Publications
Small molecules promoting protein–protein interactions produce a range of therapeutic
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

Y Hatoyama, M Islam, AG Bond, K Hayashi, A Ciulli… - EMBO …, 2024 - embopress.org
Acute protein knockdown is a powerful approach to dissecting protein function in dynamic
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 …

Degradation bottlenecks and resource competition in transiently and stably engineered mammalian cells

J Gabrielli, R Di Blasi, C Kontoravdi, F Ceroni - Nature Communications, 2025 - nature.com
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 …

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 …

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 …

[HTML][HTML] GPCR-targeted PROTACs in Cancer Therapeutics

VR Saca, T Huber, TP Sakmar - Molecular Pharmacology, 2024 - Elsevier
G protein-coupled receptors (GPCRs) comprise a family of heptahelical membrane proteins
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 …