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 through E2 recruitment
N Forte, D Dovala, MJ Hesse, JM McKenna… - ACS chemical …, 2023 - ACS Publications
Targeted protein degradation (TPD) with proteolysis targeting chimeras (PROTACs),
heterobifunctional compounds consisting of protein targeting ligands linked to recruiters of …
heterobifunctional compounds consisting of protein targeting ligands linked to recruiters of …
Electrophilic PROTACs that degrade nuclear proteins by engaging DCAF16
X Zhang, VM Crowley, TG Wucherpfennig… - Nature chemical …, 2019 - nature.com
Ligand-dependent protein degradation has emerged as a compelling strategy to
pharmacologically control the protein content of cells. So far, however, only a limited number …
pharmacologically control the protein content of cells. So far, however, only a limited number …
Small-molecule degraders beyond PROTACs—challenges and opportunities
JM Kastl, G Davies, E Godsman… - … the Science of Drug …, 2021 - journals.sagepub.com
Targeted protein degradation (TPD) is a recent strategy, utilizing the cell's proteostasis
machinery to deplete specific proteins. This represents a paradigm shift in early drug …
machinery to deplete specific proteins. This represents a paradigm shift in early drug …
Ligandability of E3 ligases for targeted protein degradation applications
Targeted protein degradation (TPD) using proteolysis targeting chimeras (PROTACs) and
molecular glue degraders has arisen as a powerful therapeutic modality for eliminating …
molecular glue degraders has arisen as a powerful therapeutic modality for eliminating …
Identification and selectivity profiling of small-molecule degraders via multi-omics approaches
NS Scholes, C Mayor-Ruiz, GE Winter - Cell Chemical Biology, 2021 - cell.com
The therapeutic modality of targeted protein degradation promises to overcome limitations of
traditional pharmacology. Small-molecule degraders recruit disease-causing proteins to E3 …
traditional pharmacology. Small-molecule degraders recruit disease-causing proteins to E3 …
Rational discovery of molecular glue degraders via scalable chemical profiling
C Mayor-Ruiz, S Bauer, M Brand, Z Kozicka… - Nature chemical …, 2020 - nature.com
Targeted protein degradation is a new therapeutic modality based on drugs that destabilize
proteins by inducing their proximity to E3 ubiquitin ligases. Of particular interest are …
proteins by inducing their proximity to E3 ubiquitin ligases. Of particular interest are …
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 …
A tale of two tails: efficient profiling of protein degraders by specific functional and target engagement readouts
AL Chernobrovkin, C Cázares-Körner… - … the Science of Drug …, 2021 - journals.sagepub.com
Targeted protein degradation represents an area of great interest, potentially offering
improvements with respect to dosing, side effects, drug resistance, and reaching …
improvements with respect to dosing, side effects, drug resistance, and reaching …
Development of targeted protein degradation therapeutics
PP Chamberlain, LG Hamann - Nature chemical biology, 2019 - nature.com
Targeted protein degradation as a therapeutic modality has seen dramatic progress and
massive investment in recent years because of the convergence of two key scientific …
massive investment in recent years because of the convergence of two key scientific …