Proteolysis-targeting chimera (PROTAC) delivery system: advancing protein degraders towards clinical translation
Y Chen, I Tandon, W Heelan, Y Wang… - Chemical Society …, 2022 - pubs.rsc.org
Proteolysis Targeting Chimeras (PROTACs), an emerging therapeutic entity designed to
degrade target proteins by hijacking the ubiquitin–proteasome system, have the potential to …
degrade target proteins by hijacking the ubiquitin–proteasome system, have the potential to …
[HTML][HTML] Bivalent ligands for protein degradation in drug discovery
M Scheepstra, KFW Hekking, L van Hijfte… - Computational and …, 2019 - Elsevier
Targeting the “undruggable” proteome remains one of the big challenges in drug discovery.
Recent innovations in the field of targeted protein degradation and manipulation of the …
Recent innovations in the field of targeted protein degradation and manipulation of the …
[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 …
Bridged proteolysis targeting chimera (PROTAC) enables degradation of undruggable targets
Proteolysis Targeting Chimeras (PROTACs) are attractive therapeutic modalities for
degrading disease-causing proteins. While many PROTACs have been developed for …
degrading disease-causing proteins. While many PROTACs have been developed for …
PROTAC-DB: an online database of PROTACs
Abstract Proteolysis-targeting chimeras (PROTACs), which selectively degrade targeted
proteins by the ubiquitin-proteasome system, have emerged as a novel therapeutic …
proteins by the ubiquitin-proteasome system, have emerged as a novel therapeutic …
Lessons in PROTAC design from selective degradation with a promiscuous warhead
Inhibiting protein function selectively is a major goal of modern drug discovery. Here, we
report a previously understudied benefit of small molecule proteolysis-targeting chimeras …
report a previously understudied benefit of small molecule proteolysis-targeting chimeras …
PROTAC-DB 2.0: an updated database of PROTACs
Proteolysis targeting chimeras (PROTACs), which harness the ubiquitin-proteasome system
to selectively induce targeted protein degradation, represent an emerging therapeutic …
to selectively induce targeted protein degradation, represent an emerging therapeutic …
Opportunities and challenges of protein-based targeted protein degradation
F Shen, LMK Dassama - Chemical Science, 2023 - pubs.rsc.org
In the 20 years since the first report of a proteolysis targeting chimeric (PROTAC) molecule,
targeted protein degradation (TPD) technologies have attempted to revolutionize the fields …
targeted protein degradation (TPD) technologies have attempted to revolutionize the fields …
[HTML][HTML] Emerging protein degradation strategies: expanding the scope to extracellular and membrane proteins
J Lin, J Jin, Y Shen, L Zhang, G Gong, H Bian… - Theranostics, 2021 - ncbi.nlm.nih.gov
Classic small molecule inhibitors that directly target pathogenic proteins typically rely on the
accessible binding sites to achieve prolonged occupancy and influence protein functions …
accessible binding sites to achieve prolonged occupancy and influence protein functions …
Proteolysis targeting chimeras (PROTACs) in cancer therapy
A Ocaña, A Pandiella - Journal of Experimental & Clinical Cancer …, 2020 - Springer
Exploitation of the protein degradation machinery as a therapeutic strategy to degrade
oncogenic proteins is experiencing revolutionary advances with the development of …
oncogenic proteins is experiencing revolutionary advances with the development of …