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Only 15% of human kinases carry a bulky residue at the DFG-1 position, providing an opportunity for the design of selective ATP-site inhibitors without the typical hinge-binding interactions. The low… Click to show full abstract
Only 15% of human kinases carry a bulky residue at the DFG-1 position, providing an opportunity for the design of selective ATP-site inhibitors without the typical hinge-binding interactions. The low sequence homology among unrelated kinases with bulky DFG-1 residues provides a new paradigm for selective kinase inhibitor development.
Keywords:
dfg binding;
kinase;
binding new;
new residue;
selective kinase;
residue developing
Journal Title: Journal of medicinal chemistry
Year Published: 2020
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Journal Title: Journal of medicinal chemistry
Year Published: 2020
Link to full text (if available)
Share on Social Media: Sign Up to like & get
recommendations!