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

Erik B. Faber; Gunda I. Georg

doi:10.1021/acs.jmedchem.0c01501

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

Erik B. Faber, Gunda I. Georg

Medicinal Chemistry

Research output: Contribution to journal › Review article › peer-review

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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)
Pages (from-to)	10221-10223
Number of pages	3
Journal	Journal of medicinal chemistry
Volume	63
Issue number	18
DOIs	https://doi.org/10.1021/acs.jmedchem.0c01501
State	Published - Sep 24 2020

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title = "DFG-1 Binding: A New Residue for Developing Selective Kinase Inhibitors",

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. ",

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AU - Georg, Gunda I.

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AB - 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.

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

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