MPS1 kinase with 3-aminopyridin-2-one inhibitorsMPS1 kinase with 3-aminopyridin-2-one inhibitors

Structural highlights

4cv8 is a 1 chain structure. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:,
Activity:Dual-specificity kinase, with EC number 2.7.12.1
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

[TTK_HUMAN] Phosphorylates proteins on serine, threonine, and tyrosine. Probably associated with cell proliferation. Essential for chromosome alignment by enhancing AURKB activity (via direct CDCA8 phosphorylation) at the centromere, and for the mitotic checkpoint.[1]

References

  1. Jelluma N, Brenkman AB, van den Broek NJ, Cruijsen CW, van Osch MH, Lens SM, Medema RH, Kops GJ. Mps1 phosphorylates Borealin to control Aurora B activity and chromosome alignment. Cell. 2008 Jan 25;132(2):233-46. doi: 10.1016/j.cell.2007.11.046. PMID:18243099 doi:10.1016/j.cell.2007.11.046

4cv8, resolution 3.00Å

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