An overview of PROTACs: a promising drug discovery paradigm
Z Liu, M Hu, Y Yang, C Du, H Zhou, C Liu, Y Chen… - Molecular …, 2022 - Springer
Proteolysis targeting chimeras (PROTACs) technology has emerged as a novel therapeutic
paradigm in recent years. PROTACs are heterobifunctional molecules that degrade target …
paradigm in recent years. PROTACs are heterobifunctional molecules that degrade target …
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 …
PROTAC degraders as chemical probes for studying target biology and target validation
Small molecule degraders such as PROTACs (PROteolysis TArgeting Chimeras) have
emerged as new promising pharmacological modalities and the first PROTAC drug …
emerged as new promising pharmacological modalities and the first PROTAC drug …
The state of the art of PROTAC technologies for drug discovery
C Wang, C Zheng, H Wang, L Zhang, Z Liu… - European Journal of …, 2022 - Elsevier
Protein degradation technology has progressed dramatically since 2001 when proteolysis
targeting chimera (PROTAC) was first reported. Various of distinctive degradation …
targeting chimera (PROTAC) was first reported. Various of distinctive degradation …
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 …
Assays and technologies for developing proteolysis targeting chimera degraders
Targeted protein degradation by small-molecule degraders represents an emerging mode of
action in drug discovery. Proteolysis targeting chimeras (PROTACs) are small molecules …
action in drug discovery. Proteolysis targeting chimeras (PROTACs) are small molecules …
[HTML][HTML] Proteomic approaches advancing targeted protein degradation
G Sathe, GP Sapkota - Trends in pharmacological sciences, 2023 - cell.com
Targeted protein degradation (TPD) is an emerging modality for research and therapeutics.
Most TPD approaches harness cellular ubiquitin-dependent proteolytic pathways …
Most TPD approaches harness cellular ubiquitin-dependent proteolytic pathways …
Chemistries of bifunctional PROTAC degraders
C Cao, M He, L Wang, Y He, Y Rao - Chemical Society Reviews, 2022 - pubs.rsc.org
Proteolysis targeting chimeras (PROTACs) technology is a novel and promising therapeutic
strategy using small molecules to induce ubiquitin-dependent degradation of proteins. It has …
strategy using small molecules to induce ubiquitin-dependent degradation of proteins. It has …
Proteolysis-targeting chimeras (PROTACs) in cancer therapy
X Li, W Pu, Q Zheng, M Ai, S Chen, Y Peng - Molecular cancer, 2022 - Springer
Proteolysis-targeting chimeras (PROTACs) are engineered techniques for targeted protein
degradation. A bifunctional PROTAC molecule with two covalently-linked ligands recruits …
degradation. A bifunctional PROTAC molecule with two covalently-linked ligands recruits …
PROTACs: great opportunities for academia and industry
X Sun, H Gao, Y Yang, M He, Y Wu, Y Song… - Signal transduction and …, 2019 - nature.com
Although many kinds of therapies are applied in the clinic, drug-resistance is a major and
unavoidable problem. Another disturbing statistic is the limited number of drug targets, which …
unavoidable problem. Another disturbing statistic is the limited number of drug targets, which …