Reference: Lu, W. et al. Fragment-based covalent ligand discovery. Rsc Chem Biology (2021) doi:10.1039/d0cb00222d
https://pubs.rsc.org/en/content/articlelanding/2021/cb/d0cb00222d
Fragment-based covalent ligand discovery
Targeted covalent inhibitors have regained widespread attention in drug discovery and have emerged as powerful tools for basic biomedical research. Fueled by considerable improvements in mass spectrometry sensitivity and sample processing, chemoproteomic s
pubs.rsc.org
@Strategies for covalent fragment discovery
-Target-based covalent fragment discovery
-Cell-based covalent fragment discovery
-Photoactivation-assisted fragment discovery
@Computer-aided covalent fragment design
@Advanced challenging pharmacoloigcal modalities
-Inhibition of protein-protein interactions
-Covalent fragments for allosteric regulator development
-Development of proteolysis targetic chimeras (PROTACs)
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