6gvj

Human Mps1 kinase domain with ordered activation loop

spinqualitylabelsall models 6gvj, resolution 2.41Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 6gvj is a 1 chain structure with sequence from Human. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: CL, GOL Gene: TTK, MPS1, MPS1L1 (HUMAN) 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. Publication Abstract from PubMed Monopolar spindle 1 (Mps1) is a dual-specificity protein kinase, orchestrating faithful chromosome segregation during mitosis. All reported structures of the Mps1 kinase adopt the hallmarks of an inactive conformation, which includes a mostly disordered activation loop. Here we present a 2.4A resolution crystal structure of an 'extended' version of the Mps1 kinase domain, which shows an ordered activation loop. However, the other structural characteristics of an active kinase are not present. Our structure shows that the Mps1 activation loop can fit to the ATP binding pocket and interferes with ATP, but less so with inhibitors binding, partly explain the potency of various Mps1 inhibitors. This article is protected by copyright. All rights reserved. A crystal structure of the human protein kinase Mps1 reveals an ordered conformation of the activation loop.,Roorda JC, Joosten RP, Perrakis A, Hiruma Y Proteins. 2018 Dec 23. doi: 10.1002/prot.25651. PMID:30582207 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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