Targeted Protein Degradation through Recruitment of the CUL4 Complex Adaptor Protein DDB1
M Meyers, S Cismoski, A Panidapu… - ACS chemical …, 2024 - ACS Publications
Targeted protein degradation has arisen as a powerful therapeutic modality for eliminating
proteins. Thus far, most heterobifunctional proteolysis targeting chimeras (PROTACs) have …
proteins. Thus far, most heterobifunctional proteolysis targeting chimeras (PROTACs) have …
Targeted degradation via direct 26S proteasome recruitment
C Bashore, S Prakash, MC Johnson… - Nature Chemical …, 2023 - nature.com
Engineered destruction of target proteins by recruitment to the cell's degradation machinery
has emerged as a promising strategy in drug discovery. The majority of molecules that …
has emerged as a promising strategy in drug discovery. The majority of molecules that …
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 …
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 …
Molecular glues for targeted protein degradation: from serendipity to rational discovery
Targeted protein degradation is a promising area in the discovery and development of
innovative therapeutics. Molecular glues mediate proximity-induced protein degradation and …
innovative therapeutics. Molecular glues mediate proximity-induced protein degradation and …
Discovery of molecular glue degraders via isogenic morphological profiling
A Ng, F Offensperger, JA Cisneros… - ACS Chemical …, 2023 - ACS Publications
Molecular glue degraders (MGDs) are small molecules that degrade proteins of interest via
the ubiquitin–proteasome system. While MGDs were historically discovered serendipitously …
the ubiquitin–proteasome system. While MGDs were historically discovered serendipitously …
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 …
In vivo target protein degradation induced by PROTACs based on E3 ligase DCAF15
L Li, D Mi, H Pei, Q Duan, X Wang, W Zhou… - … and Targeted Therapy, 2020 - nature.com
As an emerging drug discovery paradigm, Proteolysis targeting chimeras (PROTACs)
facilitate ubiquitination and degradation of the targets by cellular endogenous proteasome …
facilitate ubiquitination and degradation of the targets by cellular endogenous proteasome …
DCAF11 supports targeted protein degradation by electrophilic proteolysis-targeting chimeras
X Zhang, LM Luukkonen, CL Eissler… - Journal of the …, 2021 - ACS Publications
Ligand-induced protein degradation has emerged as a compelling approach to promote the
targeted elimination of proteins from cells by directing these proteins to the ubiquitin …
targeted elimination of proteins from cells by directing these proteins to the ubiquitin …
Degradation of the BAF complex factor BRD9 by heterobifunctional ligands
D Remillard, DL Buckley, J Paulk… - Angewandte Chemie …, 2017 - Wiley Online Library
The bromodomain‐containing protein BRD9, a subunit of the human BAF (SWI/SNF)
nucleosome remodeling complex, has emerged as an attractive therapeutic target in cancer …
nucleosome remodeling complex, has emerged as an attractive therapeutic target in cancer …