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3vap
From Proteopedia
(Difference between revisions)
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==Synthesis and SAR Studies of imidazo-[1,2-a]-pyrazine Aurora kinase inhibitors with improved off target kinase selectivity== | ==Synthesis and SAR Studies of imidazo-[1,2-a]-pyrazine Aurora kinase inhibitors with improved off target kinase selectivity== | ||
<StructureSection load='3vap' size='340' side='right' caption='[[3vap]], [[Resolution|resolution]] 2.66Å' scene=''> | <StructureSection load='3vap' size='340' side='right' caption='[[3vap]], [[Resolution|resolution]] 2.66Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>[[3vap]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/ | + | <table><tr><td colspan='2'>[[3vap]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3VAP OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3VAP FirstGlance]. <br> |
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=0FY:3-(1-{2-[(3-FLUOROPYRIDINIUM-4-YL)AMINO]-2-OXOETHYL}-1H-PYRAZOL-4-YL)-6-METHYL-8-[(3-{[(1R,3R)-3-METHYLPIPERIDINIUM-1-YL]METHYL}-1,2-THIAZOL-5-YL)AMINO]IMIDAZO[1,2-A]PYRAZIN-1-IUM'>0FY</scene></td></tr> | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=0FY:3-(1-{2-[(3-FLUOROPYRIDINIUM-4-YL)AMINO]-2-OXOETHYL}-1H-PYRAZOL-4-YL)-6-METHYL-8-[(3-{[(1R,3R)-3-METHYLPIPERIDINIUM-1-YL]METHYL}-1,2-THIAZOL-5-YL)AMINO]IMIDAZO[1,2-A]PYRAZIN-1-IUM'>0FY</scene></td></tr> | ||
| - | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">AURKA, AIK, AIRK1, ARK1, AURA, AYK1, BTAK, IAK1, STK15, STK6 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 | + | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">AURKA, AIK, AIRK1, ARK1, AURA, AYK1, BTAK, IAK1, STK15, STK6 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr> |
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </span></td></tr> | <tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </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=3vap FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3vap OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3vap RCSB], [http://www.ebi.ac.uk/pdbsum/3vap PDBsum]</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=3vap FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3vap OCA], [http://pdbe.org/3vap PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=3vap RCSB], [http://www.ebi.ac.uk/pdbsum/3vap PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=3vap ProSAT]</span></td></tr> |
</table> | </table> | ||
== Function == | == Function == | ||
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
</div> | </div> | ||
| + | <div class="pdbe-citations 3vap" style="background-color:#fffaf0;"></div> | ||
==See Also== | ==See Also== | ||
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__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
| - | [[Category: | + | [[Category: Human]] |
[[Category: Non-specific serine/threonine protein kinase]] | [[Category: Non-specific serine/threonine protein kinase]] | ||
[[Category: Basso, A D]] | [[Category: Basso, A D]] | ||
Revision as of 12:09, 5 August 2016
Synthesis and SAR Studies of imidazo-[1,2-a]-pyrazine Aurora kinase inhibitors with improved off target kinase selectivity
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