4c4h

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'''Unreleased structure'''
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{{STRUCTURE_4c4h| PDB=4c4h | SCENE= }}
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===Structure-based design of orally bioavailable pyrrolopyridine inhibitors of the mitotic kinase MPS1===
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{{ABSTRACT_PUBMED_24256217}}
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The entry 4c4h is ON HOLD until Paper Publication
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==Function==
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[[http://www.uniprot.org/uniprot/TTK_HUMAN 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.<ref>PMID:18243099</ref>
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Authors: Naud, S., Westwood, I.M., Faisal, A., Sheldrake, P., Bavetsias, V., Atrash, B., 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., Eccles, S.A., Raynaud, F.I., Linardopoulos, S., van Montfort, R., Blagg, J.
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==About this Structure==
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[[4c4h]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4C4H OCA].
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Description: Structure-based design of orally bioavailable pyrrolopyridine inhibitors of the mitotic kinase MPS1
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==Reference==
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<ref group="xtra">PMID:024256217</ref><references group="xtra"/><references/>
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[[Category: Dual-specificity kinase]]
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[[Category: Atrash, B.]]
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[[Category: Baker, R.]]
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[[Category: Bavetsias, V.]]
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[[Category: Blagg, J.]]
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[[Category: Boxall, K.]]
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[[Category: Brandon, A de Haven.]]
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[[Category: Burke, R.]]
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[[Category: Choi, V.]]
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[[Category: Eccles, S A.]]
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[[Category: Faisal, A.]]
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[[Category: Gurden, M.]]
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[[Category: Hayes, A.]]
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[[Category: Henley, A.]]
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[[Category: Linardopoulos, S.]]
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[[Category: Liu, M.]]
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[[Category: Mak, G.]]
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[[Category: Matijssen, B.]]
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[[Category: McAndrew, C.]]
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[[Category: Montfort, R van.]]
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[[Category: Naud, S.]]
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[[Category: Raynaud, F I.]]
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[[Category: Schmitt, J.]]
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[[Category: Sheldrake, P.]]
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[[Category: Valenti, M.]]
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[[Category: Westwood, I M.]]
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[[Category: Wood, A.]]
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[[Category: Mitosis]]
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[[Category: Protein kinase]]
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[[Category: Structure-based design]]
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[[Category: Transferase]]

Revision as of 07:25, 4 December 2013

Template:STRUCTURE 4c4h

Contents

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

Template:ABSTRACT PUBMED 24256217

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]

About this Structure

4c4h is a 1 chain structure. Full crystallographic information is available from OCA.

Reference

  • 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
  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

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