[HTML][HTML] Monitoring and deciphering protein degradation pathways inside cells
A new series of therapeutic modalities resulting in degradation of target proteins, termed
proteolysis targeting chimeras (PROTACs), hold significant therapeutic potential with …
proteolysis targeting chimeras (PROTACs), hold significant therapeutic potential with …
Targeted protein degradation: elements of PROTAC design
SL Paiva, CM Crews - Current opinion in chemical biology, 2019 - Elsevier
Targeted protein degradation using Proteolysis Targeting Chimeras (PROTACs) has
emerged as a novel therapeutic modality in drug discovery. PROTACs mediate the …
emerged as a novel therapeutic modality in drug discovery. PROTACs mediate the …
Exploring the target scope of KEAP1 E3 ligase-based PROTACs
Targeted protein degradation (TPD) uses small molecules to recruit E3 ubiquitin ligases into
the proximity of proteins of interest, inducing ubiquitination-dependent degradation. A major …
the proximity of proteins of interest, inducing ubiquitination-dependent degradation. A major …
Molecular recognition of ternary complexes: a new dimension in the structure-guided design of chemical degraders
Molecular glues and bivalent inducers of protein degradation (also known as PROTACs)
represent a fascinating new modality in pharmacotherapeutics: the potential to knockdown …
represent a fascinating new modality in pharmacotherapeutics: the potential to knockdown …
PROTAC-DB: an online database of PROTACs
Abstract Proteolysis-targeting chimeras (PROTACs), which selectively degrade targeted
proteins by the ubiquitin-proteasome system, have emerged as a novel therapeutic …
proteins by the ubiquitin-proteasome system, have emerged as a novel therapeutic …
Identification and optimization of molecular glue compounds that inhibit a noncovalent E2 enzyme–ubiquitin complex
Pharmacological control of the ubiquitin-proteasome system (UPS) is of intense interest in
drug discovery. Here, we report the development of chemical inhibitors of the ubiquitin …
drug discovery. Here, we report the development of chemical inhibitors of the ubiquitin …
Rational chemical design of molecular glue degraders
ES Toriki, JW Papatzimas, K Nishikawa… - ACS central …, 2023 - ACS Publications
Targeted protein degradation with molecular glue degraders has arisen as a powerful
therapeutic modality for eliminating classically undruggable disease-causing proteins …
therapeutic modality for eliminating classically undruggable disease-causing proteins …
Catalytic in vivo protein knockdown by small-molecule PROTACs
DP Bondeson, A Mares, IED Smith, E Ko… - Nature chemical …, 2015 - nature.com
The current predominant therapeutic paradigm is based on maximizing drug-receptor
occupancy to achieve clinical benefit. This strategy, however, generally requires excessive …
occupancy to achieve clinical benefit. This strategy, however, generally requires excessive …
Harnessing the E3 ligase KEAP1 for targeted protein degradation
Proteolysis targeting chimeras (PROTACs) represent a new class of promising therapeutic
modalities. PROTACs hijack E3 ligases and the ubiquitin-proteasome system (UPS), leading …
modalities. PROTACs hijack E3 ligases and the ubiquitin-proteasome system (UPS), leading …
Small‐molecule control of intracellular protein levels through modulation of the ubiquitin proteasome system
DL Buckley, CM Crews - Angewandte Chemie International …, 2014 - Wiley Online Library
Traditionally, biological probes and drugs have targeted the activities of proteins (such as
enzymes and receptors) that can be readily controlled by small molecules. The remaining …
enzymes and receptors) that can be readily controlled by small molecules. The remaining …