4c4j
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
Template:ABSTRACT PUBMED 24256217
FunctionFunction
[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]
About this StructureAbout this Structure
4c4j is a 1 chain structure with sequence from Human. Full crystallographic information is available from OCA.
ReferenceReference
- ↑ Naud S, Westwood IM, Faisal A, Sheldrake P, Bavetsias V, Atrash B, Cheung KM, Liu M, Hayes A, Schmitt J, Wood A, Choi V, Boxall K, Mak G, Gurden M, Valenti M, de Haven Brandon A, Henley A, Baker R, McAndrew C, Matijssen B, Burke R, Hoelder S, Eccles SA, Raynaud FI, Linardopoulos S, van Montfort RL, Blagg J. Structure-Based Design of Orally Bioavailable 1H-Pyrrolo[3,2-c]pyridine Inhibitors of Mitotic Kinase Monopolar Spindle 1 (MPS1). J Med Chem. 2013 Dec 2. PMID:24256217 doi:http://dx.doi.org/10.1021/jm401395s
- ↑ 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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OCACategories:
- Dual-specificity kinase
- Human
- Atrash, B.
- Baker, R.
- Bavetsias, V.
- Blagg, J.
- Boxall, K.
- Brandon, A de Haven.
- Burke, R.
- Choi, V.
- Eccles, S A.
- Faisal, A.
- Gurden, M.
- Hayes, A.
- Henley, A.
- Linardopoulos, S.
- Liu, M.
- Mak, G.
- Matijssen, B.
- McAndrew, C.
- Montfort, R van.
- Naud, S.
- Raynaud, F I.
- Schmitt, J.
- Sheldrake, P.
- Valenti, M.
- Westwood, I M.
- Wood, A.
- Mitosis
- Structure-based drug design
- Transferase