Proteolysis targeting chimeras (PROTACs) are emerging therapeutics for hematologic malignancies

Y He, S Khan, Z Huo, D Lv, X Zhang, X Liu… - Journal of Hematology & …, 2020 - Springer
Proteolysis targeting chimeras (PROTACs) are heterobifunctional small molecules that
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 …

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 …

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 …

Cancer selective target degradation by folate-caged PROTACs

J Liu, H Chen, Y Liu, Y Shen, F Meng… - Journal of the …, 2021 - ACS Publications
PROTACs (proteolysis targeting chimeras) are an emerging class of promising therapeutic
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 …

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 …

Induced protein degradation: an emerging drug discovery paradigm

AC Lai, CM Crews - Nature reviews Drug discovery, 2017 - nature.com
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 …

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 …

Tracking the PROTAC degradation pathway in living cells highlights the importance of ternary complex measurement for PROTAC optimization

MP Schwalm, A Krämer, A Dölle, J Weckesser, X Yu… - Cell chemical …, 2023 - cell.com
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 …