Discovery of a novel allosteric inhibitor-binding site in ERK5: comparison with the canonical kinase hinge ATP-binding site
Crystal structures of the MAP kinase ERK5 in complex with XMD8-92 and four novel inhibitors reveal an allosteric binding site between the kinase P-loop and αC helix. Binding at this site displaces the P-loop into the ATP-binding site and was shown to be ATP-competitive.
| Main Authors: | , , , , , , , , , |
|---|---|
| Format: | Online |
| Language: | English |
| Published: |
International Union of Crystallography
2016
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| Online Access: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4854315/ |