Article
Nek7 conformational flexibility and inhibitor binding probed through protein engineering of the R-spine.
The Biochemical journal - 30 Apr 2020
Byrne Matthew J, Nasir Nazia, Basmadjian Christine, Bhatia Chitra, Cunnison Rory F, Carr Katherine H, Mas-Droux Corine, Yeoh Sharon, Cano Céline, Bayliss Richard
Abstract excerpt
Nek7 is a serine/threonine-protein kinase required for proper spindle formation and cytokinesis. Elevated Nek7 levels have been observed in several cancers, and inhibition of Nek7 might provide a route to the development of cancer therapeutics. To date, no selective and potent Nek7 inhibitors have been identified. Nek7 crystal structures exhibit an improperly formed regulatory-spine (R-spine), characteristic of...
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