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.
Original language | English (US) |
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Pages (from-to) | 10221-10223 |
Number of pages | 3 |
Journal | Journal of medicinal chemistry |
Volume | 63 |
Issue number | 18 |
DOIs | |
State | Published - Sep 24 2020 |
PubMed: MeSH publication types
- Journal Article
- Comment