Proteolysis targeting chimeras (PROTACs) are emerging therapeutics for hematologic malignancies
Proteolysis targeting chimeras (PROTACs) are heterobifunctional small molecules that
utilize the ubiquitin proteasome system (UPS) to degrade proteins of interest (POI) …
utilize the ubiquitin proteasome system (UPS) to degrade proteins of interest (POI) …
PROTAC: A promising technology for cancer treatment
X Zhou, R Dong, JY Zhang, X Zheng, LP Sun - European journal of …, 2020 - Elsevier
Proteolysis-targeting chimeric molecules (PROTACs), which attract much more attention
today, may be a potential way to treat cancer. PROTACs are made up of ligands of target …
today, may be a potential way to treat cancer. PROTACs are made up of ligands of target …
Proteolysis-targeting chimeras as therapeutics and tools for biological discovery
GM Burslem, CM Crews - Cell, 2020 - cell.com
New biological tools provide new techniques to probe fundamental biological processes.
Here we describe the burgeoning field of proteolysis-targeting chimeras (PROTACs), which …
Here we describe the burgeoning field of proteolysis-targeting chimeras (PROTACs), which …
Small‐molecule PROTACS: new approaches to protein degradation
M Toure, CM Crews - Angewandte Chemie International …, 2016 - Wiley Online Library
The current inhibitor‐based approach to therapeutics has inherent limitations owing to its
occupancy‐based model: 1) there is a need to maintain high systemic exposure to ensure …
occupancy‐based model: 1) there is a need to maintain high systemic exposure to ensure …
Cancer selective target degradation by folate-caged PROTACs
PROTACs (proteolysis targeting chimeras) are an emerging class of promising therapeutic
modalities that degrade intracellular protein targets by hijacking the cellular ubiquitin …
modalities that degrade intracellular protein targets by hijacking the cellular ubiquitin …
Clinical considerations for the design of PROTACs in cancer
C Nieto-Jiménez, EC Morafraile, C Alonso-Moreno… - Molecular Cancer, 2022 - Springer
Degradation of targeted proteins using proteolysis targeting chimeras (PROTACs) has
gained momentum. A PROTAC is a bifunctional molecule that consists of three parts: a …
gained momentum. A PROTAC is a bifunctional molecule that consists of three parts: a …
Antibody–PROTAC conjugates enable HER2-dependent targeted protein degradation of BRD4
M Maneiro, N Forte, MM Shchepinova… - ACS chemical …, 2020 - ACS Publications
Targeting protein degradation with Proteolysis-Targeting Chimeras (PROTACs) is an area of
great current interest in drug discovery. Nevertheless, although the high effectiveness of …
great current interest in drug discovery. Nevertheless, although the high effectiveness of …
Induced protein degradation: an emerging drug discovery paradigm
Small-molecule drug discovery has traditionally focused on occupancy of a binding site that
directly affects protein function, and this approach typically precludes targeting proteins that …
directly affects protein function, and this approach typically precludes targeting proteins that …
Cell morphological profiling enables high-throughput screening for PROteolysis TArgeting Chimera (PROTAC) phenotypic signature
MA Trapotsi, E Mouchet, G Williams… - ACS Chemical …, 2022 - ACS Publications
PROteolysis TArgeting Chimeras (PROTACs) use the ubiquitin–proteasome system to
degrade a protein of interest for therapeutic benefit. Advances made in targeted protein …
degrade a protein of interest for therapeutic benefit. Advances made in targeted protein …
Tracking the PROTAC degradation pathway in living cells highlights the importance of ternary complex measurement for PROTAC optimization
The multi-step degradation process of PROteolysis TArgeting Chimeras (PROTACs) poses a
challenge for their rational development, as the rate-limiting steps that determine PROTACs …
challenge for their rational development, as the rate-limiting steps that determine PROTACs …