[HTML][HTML] PROteolysis TArgeting Chimeras (PROTACs)—past, present and future
M Pettersson, CM Crews - Drug Discovery Today: Technologies, 2019 - Elsevier
The majority of currently used therapeutics are small molecule-based and utilize occupancy-
driven pharmacology as the mode of action (MOA), in which the protein function is …
driven pharmacology as the mode of action (MOA), in which the protein function is …
PROTAC technology: opportunities and challenges
H Gao, X Sun, Y Rao - ACS medicinal chemistry letters, 2020 - ACS Publications
PROTACs-induced targeted protein degradation has emerged as a novel therapeutic
strategy in drug development and attracted the favor of academic institutions, large …
strategy in drug development and attracted the favor of academic institutions, large …
PROTACs: an emerging targeting technique for protein degradation in drug discovery
S Gu, D Cui, X Chen, X Xiong, Y Zhao - BioEssays, 2018 - Wiley Online Library
Proteolysis‐targeting chimeric molecules (PROTACs) represent an emerging technique that
is receiving much attention for therapeutic intervention. The mechanism is based on the …
is receiving much attention for therapeutic intervention. The mechanism is based on the …
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 …
Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs
S An, L Fu - EBioMedicine, 2018 - thelancet.com
There are several challenges towards the development and clinical use of small molecule
inhibitors, which are currently the main type of targeted therapies towards intracellular …
inhibitors, which are currently the main type of targeted therapies towards intracellular …
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 …
Enzyme-catalyzed activation of pro-PROTAC for cell-selective protein degradation
C Liang, Q Zheng, T Luo, W Cai, L Mao… - CCS …, 2022 - chinesechemsoc.org
Proteolysis targeting chimera (PROTAC) technology is a chemical protein knockdown
approach that degrades protein by hijacking the cellular ubiquitin-proteasome system to …
approach that degrades protein by hijacking the cellular ubiquitin-proteasome system to …
[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 …
Quantitative live-cell kinetic degradation and mechanistic profiling of PROTAC mode of action
A new generation of heterobifunctional small molecules, termed proteolysis targeting
chimeras (PROTACs), targets proteins for degradation through recruitment to E3 ligases and …
chimeras (PROTACs), targets proteins for degradation through recruitment to E3 ligases and …
Opportunities and challenges of small molecule induced targeted protein degradation
M He, W Lv, Y Rao - Frontiers in Cell and Developmental Biology, 2021 - frontiersin.org
Proteolysis targeting chimeras (PROTAC) represents a new type of small molecule induced
protein degradation technology that has emerged in recent years. PROTAC uses …
protein degradation technology that has emerged in recent years. PROTAC uses …