5eh0
From Proteopedia
(Difference between revisions)
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==Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle kinase 1 (MPS1) Using a Structure-Based Hydridization Approach== | ==Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle kinase 1 (MPS1) Using a Structure-Based Hydridization Approach== | ||
| - | <StructureSection load='5eh0' size='340' side='right' caption='[[5eh0]], [[Resolution|resolution]] 2.18Å' scene=''> | + | <StructureSection load='5eh0' size='340' side='right'caption='[[5eh0]], [[Resolution|resolution]] 2.18Å' scene=''> |
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>[[5eh0]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5EH0 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5EH0 FirstGlance]. <br> | + | <table><tr><td colspan='2'>[[5eh0]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Synthetic_construct_sequences Synthetic construct sequences]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5EH0 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5EH0 FirstGlance]. <br> |
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=5NW:N2-(2-METHOXY-4-(1-METHYL-1H-PYRAZOL-4-YL)PHENYL)-N8-NEOPENTYLPYRIDO[3,4-D]PYRIMIDINE-2,8-DIAMINE'>5NW</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene></td></tr> | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=5NW:N2-(2-METHOXY-4-(1-METHYL-1H-PYRAZOL-4-YL)PHENYL)-N8-NEOPENTYLPYRIDO[3,4-D]PYRIMIDINE-2,8-DIAMINE'>5NW</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene></td></tr> | ||
| + | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">TTK, MPS1, MPS1L1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=32630 SYNTHETIC CONSTRUCT sequences])</td></tr> | ||
| + | <tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Dual-specificity_kinase Dual-specificity kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.12.1 2.7.12.1] </span></td></tr> | ||
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5eh0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5eh0 OCA], [http://pdbe.org/5eh0 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5eh0 RCSB], [http://www.ebi.ac.uk/pdbsum/5eh0 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5eh0 ProSAT]</span></td></tr> | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5eh0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5eh0 OCA], [http://pdbe.org/5eh0 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5eh0 RCSB], [http://www.ebi.ac.uk/pdbsum/5eh0 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5eh0 ProSAT]</span></td></tr> | ||
</table> | </table> | ||
| + | == Function == | ||
| + | [[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> | ||
<div style="background-color:#fffaf0;"> | <div style="background-color:#fffaf0;"> | ||
== Publication Abstract from PubMed == | == Publication Abstract from PubMed == | ||
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</div> | </div> | ||
<div class="pdbe-citations 5eh0" style="background-color:#fffaf0;"></div> | <div class="pdbe-citations 5eh0" style="background-color:#fffaf0;"></div> | ||
| + | |||
| + | ==See Also== | ||
| + | *[[Dual specificity protein kinase|Dual specificity protein kinase]] | ||
== References == | == References == | ||
<references/> | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
| + | [[Category: Dual-specificity kinase]] | ||
| + | [[Category: Large Structures]] | ||
| + | [[Category: Synthetic construct sequences]] | ||
[[Category: Baker, R]] | [[Category: Baker, R]] | ||
[[Category: Blagg, J]] | [[Category: Blagg, J]] | ||
Revision as of 07:34, 24 April 2019
Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle kinase 1 (MPS1) Using a Structure-Based Hydridization Approach
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Categories: Dual-specificity kinase | Large Structures | Synthetic construct sequences | Baker, R | Blagg, J | Box, G | Brandon, A De Haven | Burke, R | Cronin, N | Eccles, S A | Faisal, A | Fee, L O | Hayes, A | Henley, A T | Hoelder, S | Innocenti, P | Linardopoulos, S | Mak, G | Montfort, R L.M van | Naud, N | Raymaud, F I | Roberts, J | Saville, J | Schmitt, J | Solanki, S | Valenti, M | Westwood, I M | Woodward, H L | Transferase
