Targeted protein degradation: mechanisms, strategies and application
L Zhao, J Zhao, K Zhong, A Tong, D Jia - Signal transduction and …, 2022 - nature.com
Traditional drug discovery mainly focuses on direct regulation of protein activity. The
development and application of protein activity modulators, particularly inhibitors, has been …
development and application of protein activity modulators, particularly inhibitors, has been …
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 …
[HTML][HTML] Inhibition of STAT3-ferroptosis negative regulatory axis suppresses tumor growth and alleviates chemoresistance in gastric cancer
S Ouyang, H Li, L Lou, Q Huang, Z Zhang, J Mo, M Li… - Redox biology, 2022 - Elsevier
Chemotherapy is still one of the principal treatments for gastric cancer, but the clinical
application of 5-FU is limited by drug resistance. Here, we demonstrate that ferroptosis …
application of 5-FU is limited by drug resistance. Here, we demonstrate that ferroptosis …
PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)
M He, C Cao, Z Ni, Y Liu, P Song, S Hao, Y He… - … and Targeted Therapy, 2022 - nature.com
Abstract PROteolysis TArgeting Chimeras (PROTACs) technology is a new protein-
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …
PROTAC: an effective targeted protein degradation strategy for cancer therapy
Proteolysis targeting chimeric (PROTAC) technology is an effective endogenous protein
degradation tool developed in recent years that can ubiquitinate the target proteins through …
degradation tool developed in recent years that can ubiquitinate the target proteins through …
[HTML][HTML] Current strategies for the design of PROTAC linkers: a critical review
RI Troup, C Fallan, MGJ Baud - Exploration of Targeted Anti-tumor …, 2020 - ncbi.nlm.nih.gov
Abstract PROteolysis TArgeting Chimeras (PROTACs) are heterobifunctional molecules
consisting of two ligands; an “anchor” to bind to an E3 ubiquitin ligase and a “warhead” to …
consisting of two ligands; an “anchor” to bind to an E3 ubiquitin ligase and a “warhead” to …
Recent update on development of small-molecule STAT3 inhibitors for cancer therapy: from phosphorylation inhibition to protein degradation
Signal transducer and activator of transcription 3 (STAT3) is a transcription factor that
regulates various biological processes, including proliferation, metastasis, angiogenesis …
regulates various biological processes, including proliferation, metastasis, angiogenesis …
E3 ligase ligand chemistries: from building blocks to protein degraders
In recent years, proteolysis-targeting chimeras (PROTACs), capable of achieving targeted
protein degradation, have proven their great therapeutic potential and usefulness as …
protein degradation, have proven their great therapeutic potential and usefulness as …
Unraveling the role of linker design in proteolysis targeting chimeras: Miniperspective
A current bottleneck in the development of proteolysis targeting chimeras (PROTACs) is the
empirical nature of linker length structure–activity relationships (SARs). A multidisciplinary …
empirical nature of linker length structure–activity relationships (SARs). A multidisciplinary …