Proteolysis targeting chimera (PROTAC) in drug discovery paradigm: Recent progress and future challenges

S Zeng, W Huang, X Zheng, Z Zhang, J Wang… - European journal of …, 2021 - Elsevier
Proteolysis targeting chimera (PROTAC), hijacking protein of interest (POI) and recruiting E3
ligase for target degradation via the ubiquitin-proteasome pathway, is a novel drug …

[HTML][HTML] Degradation of proteins by PROTACs and other strategies

Y Wang, X Jiang, F Feng, W Liu, H Sun - Acta Pharmaceutica Sinica B, 2020 - Elsevier
Blocking the biological functions of scaffold proteins and aggregated proteins is a
challenging goal. PROTAC proteolysis-targeting chimaera (PROTAC) technology may be …

Strategies toward discovery of potent and orally bioavailable proteolysis targeting chimera degraders of androgen receptor for the treatment of prostate cancer

X Han, L Zhao, W Xiang, C Qin, B Miao… - Journal of medicinal …, 2021 - ACS Publications
Proteolysis targeting chimera (PROTAC) small-molecule degraders have emerged as a
promising new type of therapeutic agents, but the design of PROTAC degraders with …

PROTAC: an effective targeted protein degradation strategy for cancer therapy

SM Qi, J Dong, ZY Xu, XD Cheng, WD Zhang… - Frontiers in …, 2021 - frontiersin.org
Proteolysis targeting chimeric (PROTAC) technology is an effective endogenous protein
degradation tool developed in recent years that can ubiquitinate the target proteins through …

[HTML][HTML] Recent advances in PROTACs for drug targeted protein research

T Yao, H Xiao, H Wang, X Xu - International Journal of Molecular …, 2022 - mdpi.com
Proteolysis-targeting chimera (PROTAC) is a heterobifunctional molecule. Typically,
PROTAC consists of two terminals which are the ligand of the protein of interest (POI) and …

Recent developments in PROTAC‐mediated protein degradation: from bench to clinic

Z Hu, CM Crews - ChemBioChem, 2022 - Wiley Online Library
Abstract Proteolysis‐targeting chimeras (PROTACs), an emerging paradigm‐shifting
technology, hijacks the ubiquitin‐proteasome system for targeted protein degradation …

Design and characterization of cereblon-mediated androgen receptor proteolysis-targeting chimeras

AD Takwale, SH Jo, YU Jeon, HS Kim, CH Shin… - European Journal of …, 2020 - Elsevier
Abstract Proteolysis-targeting chimera (PROTAC)-mediated protein degradation is a rapidly
emerging therapeutic intervention that induces the degradation of targeted proteins. Herein …

Target protein degradation by protacs: A budding cancer treatment strategy

D Choudhary, A Kaur, P Singh, G Chaudhary… - Pharmacology & …, 2023 - Elsevier
Cancer is one of the most common causes of death. So, its lethal effect increases with time.
Near about hundreds of cancers are known in humans. Cancer treatment is done to cure or …

Discovery of A031 as effective proteolysis targeting chimera (PROTAC) androgen receptor (AR) degrader for the treatment of prostate cancer

L Chen, L Han, S Mao, P Xu, X Xu, R Zhao, Z Wu… - European Journal of …, 2021 - Elsevier
Androgen receptor (AR) is an effective therapeutic target for the treatment of prostate cancer.
We report herein the design, synthesis, and biological evaluation of highly effective …

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 …