Discovery of a PROTAC targeting ALK with in vivo activity

G Yan, X Zhong, L Yue, C Pu, H Shan, S Lan… - European Journal of …, 2021 - Elsevier
… LDK378 and the antiproliferative activity to xenograft tumor … ALK degrader B3 with in vitro
and in vivo anti-cancer activities … of PROTAC BCL-XL degraders as potent anticancer agents …

[HTML][HTML] PROTAC degraders with ligands recruiting MDM2 E3 ubiquitin ligase: an updated perspective

X Han, W Wei, Y Sun - Acta materia medica, 2022 - ncbi.nlm.nih.gov
… MD-224 was found to achieve complete and durable … selectively binds to the p53 site on
the surface of MDM2 stabilizing p53 and degrading target protein with better anti-cancer activity. …

[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
… to selectively degrade target proteins. Recent progress in the … protein degradation are mostly
achieved via biomacromolecules. … and risks of this emerging PROTAC technology in clinical …

Discovery of SHP2-D26 as a first, potent, and effective PROTAC degrader of SHP2 protein

M Wang, J Lu, M Wang, CY Yang… - Journal of medicinal …, 2020 - ACS Publications
… -targeting chimera (PROTAC) concept. This work has led to the discovery of potent and
effective SHP2 degraders, exemplified by SHP2-D26. SHP2-D26 achieves DC 50 values of 6.0 …

[HTML][HTML] Development of PROTACs to address clinical limitations associated with BTK-targeted kinase inhibitors

R Arthur, B Valle-Argos, AJ Steele… - … of targeted anti-tumor …, 2020 - ncbi.nlm.nih.gov
… of a PROTAC (top) and the mechanism of PROTAC-mediated target degradation (bottom).
Interaction of the PROTAC … strongly ablated BTK degrading activity. Fluorescence resonance …

Nanoliposomal Bcl-xL proteolysis-targeting chimera enhances anti-cancer effects on cervical and breast cancer without on-target toxicities

J Zhang, B Zhang, C Pu, J Cui, K Huang… - … Composites and Hybrid …, 2023 - Springer
Bcl-xL targeted PROTAC enhanced anti-cancer effects on … can achieve tissue selectivity,
improve activity and safety, and … -encapsulated Bcl-xL degrading PROTAC was developed, …

Sulfatase-Induced In Situ Formulation of Antineoplastic Supra-PROTACs

N Chen, Z Zhang, X Liu, H Wang, RC Guo… - Journal of the …, 2024 - ACS Publications
… the prevented Bcl-xL degradation … the Bcl-xL degradation caused by the pro-Supra-PROTAC.
In addition, to confirm the capability of the pro-Supra-PROTAC to selectively degrade Bcl-xL

[HTML][HTML] Development of a novel PROTAC using the nucleic acid aptamer as a targeting ligand for tumor selective degradation of nucleolin

L Zhang, L Li, X Wang, H Liu, Y Zhang, T Xie… - … Therapy-Nucleic Acids, 2022 - cell.com
… tumor-targeting element and an anticancer therapeutic agent. … BET-PROTAC into breast
cancer cells for degrading BRD4 … -constructed PROTAC could achieve targeted antitumor activity

A selective Fibroblast Growth Factor Receptor 1/2 PROTAC degrader with antitumor activity

Y Kong, X Zhao, Z Wang, S Yuan, S Chen, S Lou… - Molecular Cancer …, 2024 - AACR
… for degrading various protein targets (24). For example, our group has 104 developed a
tissue-selective PROTAC for degrading BCL-XL … that PROTAC degrader may achieve 577 long-…

[PDF][PDF] Targeted protein degradation in cancers: Orthodox PROTACs and beyond

J Li, X Chen, A Lu, C Liang - The Innovation, 2023 - cell.com
… to specifically target BCL-xL and exhibit increased antitumor activity and reduced platelet …
A selective BCL-XL PROTAC degrader achieves safe and potent antitumor activity. Nat. Med…