4c4f

Structure-based design of orally bioavailable pyrrolopyridine inhibitors of the mitotic kinase MPS1Structure-based design of orally bioavailable pyrrolopyridine inhibitors of the mitotic kinase MPS1

Structural highlights

4c4f is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:	, , ,
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

↑ 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

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OCA

[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

[1]

4c4f

Structure-based design of orally bioavailable pyrrolopyridine inhibitors of the mitotic kinase MPS1Structure-based design of orally bioavailable pyrrolopyridine inhibitors of the mitotic kinase MPS1

Structural highlights

Function

See Also

References

Contents

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4c4f

Structure-based design of orally bioavailable pyrrolopyridine inhibitors of the mitotic kinase MPS1Structure-based design of orally bioavailable pyrrolopyridine inhibitors of the mitotic kinase MPS1

Structural highlights

Function

See Also

References

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