[HTML][HTML] Expanding the ligand spaces for E3 ligases for the design of protein degraders
Targeted protein degradation (TPD) has recently emerged as an exciting new drug modality.
However, the strategy of developing small molecule-based protein degraders has evolved …
However, the strategy of developing small molecule-based protein degraders has evolved …
Breaking Bad Proteins—Discovery Approaches and the Road to Clinic for Degraders
Proteolysis-targeting chimeras (PROTACs) describe compounds that bind to and induce
degradation of a target by simultaneously binding to a ubiquitin ligase. More generally …
degradation of a target by simultaneously binding to a ubiquitin ligase. More generally …
Large-scale chemoproteomics expedites ligand discovery and predicts ligand behavior in cells
Chemical modulation of proteins enables a mechanistic understanding of biology and
represents the foundation of most therapeutics. However, despite decades of research, 80 …
represents the foundation of most therapeutics. However, despite decades of research, 80 …
Exploiting the cullin E3 ligase adaptor protein SKP1 for targeted protein degradation
SH Hong, A Divakaran, A Osa, OW Huang… - ACS chemical …, 2024 - ACS Publications
Targeted protein degradation with proteolysis targeting chimeras (PROTACs) is a powerful
therapeutic modality for eliminating disease-causing proteins through targeted ubiquitination …
therapeutic modality for eliminating disease-causing proteins through targeted ubiquitination …
[HTML][HTML] Pervasive aggregation and depletion of host and viral proteins in response to cysteine-reactive electrophilic compounds
AR Julio, F Shikwana, C Truong, NR Burton… - BioRxiv, 2023 - ncbi.nlm.nih.gov
Protein homeostasis is tightly regulated, with damaged or misfolded proteins quickly
eliminated by the proteasome and autophagosome pathways. By co-opting these …
eliminated by the proteasome and autophagosome pathways. By co-opting these …
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 …
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 …