The application of ubiquitin ligases in the PROTAC drug design

Y Chen, J Jin - Acta Biochimica et Biophysica Sinica, 2020 - academic.oup.com
Protein ubiquitylation plays important roles in many biological activities. Protein
ubiquitylation is a unique process that is mainly controlled by ubiquitin ligases. The ubiquitin …

[HTML][HTML] Applications of protein ubiquitylation and deubiquitylation in drug discovery

Y Chen, H Xue, J Jin - Journal of Biological Chemistry, 2024 - Elsevier
The ubiquitin-proteasome system (UPS) is the major machinery mediating specific protein
turnover in eukaryotic cells. By ubiquitylating unwanted, damaged, or harmful proteins and …

E3 ligase ligand optimization of Clinical PROTACs

H Jiang, H Xiong, SX Gu, M Wang - Frontiers in Chemistry, 2023 - frontiersin.org
Proteolysis targeting chimeras (PROTACs) technology can realize the development of drugs
for non-druggable targets that are difficult to achieve with traditional small molecules, and …

Progress on small-molecule proteolysis-targeting chimeras

W Huang, B Wang, Z Zhang, C Zhang… - Future Medicinal …, 2019 - Taylor & Francis
Proteolysis-targeting chimeras (PROTACs) have received much attention for their promising
therapeutic intervention in recent years. These molecules, with the mechanism of …

PROTAC-DB: an online database of PROTACs

G Weng, C Shen, D Cao, J Gao, X Dong… - Nucleic acids …, 2021 - academic.oup.com
Abstract Proteolysis-targeting chimeras (PROTACs), which selectively degrade targeted
proteins by the ubiquitin-proteasome system, have emerged as a novel therapeutic …

PROTACs: current trends in protein degradation by proteolysis-targeting chimeras

J Madan, VK Ahuja, K Dua, S Samajdar… - BioDrugs, 2022 - Springer
In the recent past, proteolysis-targeting chimera (PROTAC) technology has received
enormous attention for its ability to overcome the limitations of protein inhibitors and its …

PROTACs: Promising approach for anticancer therapy

SD Kaur, N Bedi, D Kumar, DN Kapoor - Cancer Letters, 2023 - Elsevier
Proteolysis-targeting chimeras (PROTACs) are being developed as an effective method for
degrading cancer-related proteins by modifying the endogenous ubiquitin-proteasome …

Recent advances in targeted protein degraders as potential therapeutic agents

N Yang, B Kong, Z Zhu, F Huang, L Zhang, T Lu… - Molecular …, 2024 - Springer
Targeted protein degradation (TPD) technology has gradually become widespread in the
past 20 years, which greatly boosts the development of disease treatment. Contrary to small …

From classic medicinal chemistry to state‐of‐the‐art interdisciplinary medicine: Recent advances in proteolysis‐targeting chimeras technology

X Zhao, Y Chen, H Su, L Zhang - Interdisciplinary Medicine, 2023 - Wiley Online Library
Proteolysis‐targeting chimeras (PROTACs) is a targeted protein degradation (TPD)
technique effected by hijacking the ubiquitin‐proteasome system (UPS) of the cells. A …

Targeted protein degradation: expanding the toolbox

M Schapira, MF Calabrese, AN Bullock… - Nature reviews Drug …, 2019 - nature.com
Proteolysis-targeting chimeras (PROTACs) and related molecules that induce targeted
protein degradation by the ubiquitin–proteasome system represent a new therapeutic …