DFG-1 Binding: A New Residue for Developing Selective Kinase Inhibitors

Erik B. Faber, Gunda I. Georg

Research output: Contribution to journalReview articlepeer-review

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 languageEnglish (US)
Pages (from-to)10221-10223
Number of pages3
JournalJournal of medicinal chemistry
Volume63
Issue number18
DOIs
StatePublished - Sep 24 2020

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