3ztx - Revision history

OCA at 07:17, 18 August 2022

OCA — Thu, 18 Aug 2022 07:17:50 GMT

OCA at 06:37, 22 April 2020

OCA — Wed, 22 Apr 2020 06:37:27 GMT

←Older revision		Revision as of 06:37, 22 April 2020
Line 1:		Line 1:

	==Aurora kinase selective inhibitors identified using a Taxol-induced checkpoint sensitivity screen.==		==Aurora kinase selective inhibitors identified using a Taxol-induced checkpoint sensitivity screen.==
-	<StructureSection load='3ztx' size='340' side='right' caption='[[3ztx]], [[Resolution\|resolution]] 1.95Å' scene=''>	+	<StructureSection load='3ztx' size='340' side='right'caption='[[3ztx]], [[Resolution\|resolution]] 1.95Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[3ztx]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/African_clawed_frog African clawed frog]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3ZTX OCA]. For a <b>guided tour on the structure components</b> use [http://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=3ZTX FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[3ztx]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/African_clawed_frog African clawed frog]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3ZTX OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=3ZTX FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=ZTX:2-((4-(4-HYDROXYPIPERIDIN-1-YL)PHENYL)AMINO)-5,11-DIMETHYL-5H-BENZO[E]PYRIMIDO+[5,4-B][1,4]DIAZEPIN-6(11H)-ONE'>ZTX</scene></td></tr>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ZTX:2-((4-(4-HYDROXYPIPERIDIN-1-YL)PHENYL)AMINO)-5,11-DIMETHYL-5H-BENZO[E]PYRIMIDO+[5,4-B][1,4]DIAZEPIN-6(11H)-ONE'>ZTX</scene></td></tr>
	<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene></td></tr>		<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[2bfx\|2bfx]], [[2vgo\|2vgo]], [[2vrx\|2vrx]], [[2vgp\|2vgp]], [[2bfy\|2bfy]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[2bfx\|2bfx]], [[2vgo\|2vgo]], [[2vrx\|2vrx]], [[2vgp\|2vgp]], [[2bfy\|2bfy]]</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=3ztx FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3ztx OCA], [http://pdbe.org/3ztx PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=3ztx RCSB], [http://www.ebi.ac.uk/pdbsum/3ztx PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=3ztx ProSAT]</span></td></tr>	+	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=3ztx FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3ztx OCA], [http://pdbe.org/3ztx PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=3ztx RCSB], [http://www.ebi.ac.uk/pdbsum/3ztx PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=3ztx ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
Line 23:		Line 23:

	==See Also==		==See Also==
-	*[[Centromere protein\|Centromere protein]]	+	*[[Centromere protein 3D structure\|Centromere protein 3D structure]]
-	*[[Inner centromere protein\|Inner centromere protein]]	+	*[[Serine/threonine protein kinase 3D structures\|Serine/threonine protein kinase 3D structures]]
-	*[[Serine/threonine protein kinase\|Serine/threonine protein kinase]]	+
	== References ==		== References ==
	<references/>		<references/>
Line 31:		Line 30:
	</StructureSection>		</StructureSection>
	[[Category: African clawed frog]]		[[Category: African clawed frog]]
		+	[[Category: Large Structures]]
	[[Category: Non-specific serine/threonine protein kinase]]		[[Category: Non-specific serine/threonine protein kinase]]
	[[Category: Gray, N]]		[[Category: Gray, N]]

OCA at 11:40, 4 August 2016

OCA — Thu, 04 Aug 2016 11:40:06 GMT

←Older revision		Revision as of 11:40, 4 August 2016
Line 1:		Line 1:
		+
	==Aurora kinase selective inhibitors identified using a Taxol-induced checkpoint sensitivity screen.==		==Aurora kinase selective inhibitors identified using a Taxol-induced checkpoint sensitivity screen.==
	<StructureSection load='3ztx' size='340' side='right' caption='[[3ztx]], [[Resolution\|resolution]] 1.95Å' scene=''>		<StructureSection load='3ztx' size='340' side='right' caption='[[3ztx]], [[Resolution\|resolution]] 1.95Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[3ztx]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/~~Xenopus_laevis Xenopus laevis~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3ZTX OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3ZTX FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[3ztx]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/African_clawed_frog African clawed frog]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3ZTX OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3ZTX FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=ZTX:2-((4-(4-HYDROXYPIPERIDIN-1-YL)PHENYL)AMINO)-5,11-DIMETHYL-5H-BENZO[E]PYRIMIDO+[5,4-B][1,4]DIAZEPIN-6(11H)-ONE'>ZTX</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=ZTX:2-((4-(4-HYDROXYPIPERIDIN-1-YL)PHENYL)AMINO)-5,11-DIMETHYL-5H-BENZO[E]PYRIMIDO+[5,4-B][1,4]DIAZEPIN-6(11H)-ONE'>ZTX</scene></td></tr>
	<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene></td></tr>		<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[2bfx\|2bfx]], [[2vgo\|2vgo]], [[2vrx\|2vrx]], [[2vgp\|2vgp]], [[2bfy\|2bfy]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[2bfx\|2bfx]], [[2vgo\|2vgo]], [[2vrx\|2vrx]], [[2vgp\|2vgp]], [[2bfy\|2bfy]]</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=3ztx FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3ztx OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3ztx RCSB], [http://www.ebi.ac.uk/pdbsum/3ztx 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=3ztx FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3ztx OCA], [http://pdbe.org/3ztx PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=3ztx RCSB], [http://www.ebi.ac.uk/pdbsum/3ztx PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=3ztx ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
Line 19:		Line 20:
	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 3ztx" style="background-color:#fffaf0;"></div>

	==See Also==		==See Also==
	*[[Centromere protein\|Centromere protein]]		*[[Centromere protein\|Centromere protein]]
		+	*[[Inner centromere protein\|Inner centromere protein]]
	*[[Serine/threonine protein kinase\|Serine/threonine protein kinase]]		*[[Serine/threonine protein kinase\|Serine/threonine protein kinase]]
	== References ==		== References ==
Line 27:		Line 30:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: African clawed frog]]
	[[Category: Non-specific serine/threonine protein kinase]]		[[Category: Non-specific serine/threonine protein kinase]]
-	[[Category: Xenopus laevis]]
	[[Category: Gray, N]]		[[Category: Gray, N]]
	[[Category: Kwiatkowski, N]]		[[Category: Kwiatkowski, N]]

OCA at 08:56, 25 December 2014

OCA — Thu, 25 Dec 2014 08:56:29 GMT

←Older revision		Revision as of 08:56, 25 December 2014
Line 3:		Line 3:
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[3ztx]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Xenopus_laevis Xenopus laevis]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3ZTX OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3ZTX FirstGlance]. <br>		<table><tr><td colspan='2'>[[3ztx]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Xenopus_laevis Xenopus laevis]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3ZTX OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3ZTX FirstGlance]. <br>
-	</td></tr><tr><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=ZTX:2-((4-(4-HYDROXYPIPERIDIN-1-YL)PHENYL)AMINO)-5,11-DIMETHYL-5H-BENZO[E]PYRIMIDO+[5,4-B][1,4]DIAZEPIN-6(11H)-ONE'>ZTX</scene><br>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=ZTX:2-((4-(4-HYDROXYPIPERIDIN-1-YL)PHENYL)AMINO)-5,11-DIMETHYL-5H-BENZO[E]PYRIMIDO+[5,4-B][1,4]DIAZEPIN-6(11H)-ONE'>ZTX</scene></td></tr>
-	<tr><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene></td></tr>	+	<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene></td></tr>
-	<tr><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[2bfx\|2bfx]], [[2vgo\|2vgo]], [[2vrx\|2vrx]], [[2vgp\|2vgp]], [[2bfy\|2bfy]]</td></tr>	+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[2bfx\|2bfx]], [[2vgo\|2vgo]], [[2vrx\|2vrx]], [[2vgp\|2vgp]], [[2bfy\|2bfy]]</td></tr>
-	<tr><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><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3ztx FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3ztx OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3ztx RCSB], [http://www.ebi.ac.uk/pdbsum/3ztx 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=3ztx FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3ztx OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3ztx RCSB], [http://www.ebi.ac.uk/pdbsum/3ztx PDBsum]</span></td></tr>
-	<table>	+	</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/AUKBA_XENLA AUKBA_XENLA]] Serine/threonine-protein kinase component of the chromosomal passenger complex (CPC), a complex that acts as a key regulator of mitosis. The CPC complex has essential functions at the centromere in ensuring correct chromosome alignment and segregation and is required for chromatin-induced microtubule stabilization and spindle assembly. Involved in the bipolar attachment of spindle microtubules to kinetochores and is a key regulator for the onset of cytokinesis during mitosis. Required for central/midzone spindle assembly and cleavage furrow formation. Phosphorylates 'Ser-10' of histone H3 during mitosis.<ref>PMID:12221116</ref> <ref>PMID:11350965</ref> <ref>PMID:17199039</ref> [[http://www.uniprot.org/uniprot/INCEA_XENLA INCEA_XENLA]] Component of the chromosomal passenger complex (CPC), a complex that acts as a key regulator of mitosis. The CPC complex has essential functions at the centromere in ensuring correct chromosome alignment and segregation and is required for chromatin-induced microtubule stabilization and spindle assembly. Probably acts through association with aurkb or aurkc. Seems to bind directly to microtubules.<ref>PMID:12221116</ref> <ref>PMID:17199039</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 19:		Line 21:

	==See Also==		==See Also==
		+	*[[Centromere protein\|Centromere protein]]
	*[[Serine/threonine protein kinase\|Serine/threonine protein kinase]]		*[[Serine/threonine protein kinase\|Serine/threonine protein kinase]]
	== References ==		== References ==
Line 26:		Line 29:
	[[Category: Non-specific serine/threonine protein kinase]]		[[Category: Non-specific serine/threonine protein kinase]]
	[[Category: Xenopus laevis]]		[[Category: Xenopus laevis]]
-	[[Category: Gray, N.]]	+	[[Category: Gray, N]]
-	[[Category: Kwiatkowski, N.]]	+	[[Category: Kwiatkowski, N]]
-	[[Category: Musacchio, A.]]	+	[[Category: Musacchio, A]]
-	[[Category: Villa, F.]]	+	[[Category: Villa, F]]
	[[Category: Taxol-induced checkpoint inhibitor]]		[[Category: Taxol-induced checkpoint inhibitor]]
	[[Category: Transferase]]		[[Category: Transferase]]
	[[Category: Transferase-cell cycle complex]]		[[Category: Transferase-cell cycle complex]]

OCA at 09:15, 11 June 2014

OCA — Wed, 11 Jun 2014 09:15:22 GMT

←Older revision		Revision as of 09:15, 11 June 2014
Line 1:		Line 1:
-	[[~~Image:~~3ztx.~~png~~\|~~left~~\|~~200px~~]]	+	==Aurora kinase selective inhibitors identified using a Taxol-induced checkpoint sensitivity screen.==
		+	<StructureSection load='3ztx' size='340' side='right' caption='[[3ztx]], [[Resolution\|resolution]] 1.95Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[3ztx]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Xenopus_laevis Xenopus laevis]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3ZTX OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3ZTX FirstGlance]. <br>
		+	</td></tr><tr><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=ZTX:2-((4-(4-HYDROXYPIPERIDIN-1-YL)PHENYL)AMINO)-5,11-DIMETHYL-5H-BENZO[E]PYRIMIDO+[5,4-B][1,4]DIAZEPIN-6(11H)-ONE'>ZTX</scene><br>
		+	<tr><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene></td></tr>
		+	<tr><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[2bfx\|2bfx]], [[2vgo\|2vgo]], [[2vrx\|2vrx]], [[2vgp\|2vgp]], [[2bfy\|2bfy]]</td></tr>
		+	<tr><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><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3ztx FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3ztx OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3ztx RCSB], [http://www.ebi.ac.uk/pdbsum/3ztx PDBsum]</span></td></tr>
		+	<table>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	The members of the Aurora kinase family play critical roles in the regulation of the cell cycle and mitotic spindle assembly and have been intensively investigated as potential targets for a new class of anticancer drugs. We describe a new highly potent and selective class of Aurora kinase inhibitors discovered using a phenotypic cellular screen. Optimized inhibitors display many of the hallmarks of Aurora inhibition including endoreduplication, polyploidy, and loss of cell viability in cancer cells. Structure-activity relationships with respect to kinome-wide selectivity and guided by an Aurora B co-crystal structure resulted in the identification of key selectivity determinants and discovery of a subseries with selectivity toward Aurora A. A direct comparison of biochemical and cellular profiles with respect to published Aurora inhibitors including VX-680, AZD1152, MLN8054, and a pyrimidine-based compound from Genentech demonstrates that compounds 1 and 3 will become valuable additional pharmacological probes of Aurora-dependent functions.

-	~~{{STRUCTURE_3ztx\| PDB=3ztx \| SCENE= }}~~	+	Selective aurora kinase inhibitors identified using a taxol-induced checkpoint sensitivity screen.,Kwiatkowski N, Deng X, Wang J, Tan L, Villa F, Santaguida S, Huang HC, Mitchison T, Musacchio A, Gray N ACS Chem Biol. 2012 Jan 20;7(1):185-96. Epub 2011 Oct 21. PMID:21992004<ref>PMID:21992004</ref>

-	~~===Aurora kinase selective inhibitors identified using~~ a ~~Taxol-induced checkpoint sensitivity screen~~.~~===~~	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>

-	~~{{ABSTRACT_PUBMED_21992004}}~~	+	==See Also==
-		+	*[[Serine/threonine protein kinase\|Serine/threonine protein kinase]]
-	==~~About this Structure~~==	+	== References ==
-	[[~~3ztx]] is a 4 chain structure with sequence from [http:~~//~~en.wikipedia.org/wiki/Xenopus_laevis Xenopus laevis~~]~~. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3ZTX OCA~~].	+	<references/>
-		+	__TOC__
-	==~~Reference~~==	+	</StructureSection>
-	<~~ref group="xtra">PMID:021992004<~~/~~ref~~><~~references group="xtra"~~/>	+
	[[Category: Non-specific serine/threonine protein kinase]]		[[Category: Non-specific serine/threonine protein kinase]]
	[[Category: Xenopus laevis]]		[[Category: Xenopus laevis]]

OCA at 10:25, 8 August 2012

OCA — Wed, 08 Aug 2012 10:25:54 GMT

←Older revision		Revision as of 10:25, 8 August 2012
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-	[[Image:3ztx.~~jpg~~\|left\|200px]]	+	[[Image:3ztx.png\|left\|200px]]

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	{{STRUCTURE_3ztx\| PDB=3ztx \| SCENE= }}		{{STRUCTURE_3ztx\| PDB=3ztx \| SCENE= }}

	===Aurora kinase selective inhibitors identified using a Taxol-induced checkpoint sensitivity screen.===		===Aurora kinase selective inhibitors identified using a Taxol-induced checkpoint sensitivity screen.===

-
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	{{ABSTRACT_PUBMED_21992004}}		{{ABSTRACT_PUBMED_21992004}}

OCA at 07:22, 1 February 2012

OCA — Wed, 01 Feb 2012 07:22:22 GMT

←Older revision		Revision as of 07:22, 1 February 2012
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-	~~'''Unreleased structure'''~~	+	[[Image:3ztx.jpg\|left\|200px]]

-	The ~~entry 3ztx~~ is ~~ON HOLD~~ ~~until Paper Publication~~	+	<!--
		+	The line below this paragraph, containing "STRUCTURE_3ztx", creates the "Structure Box" on the page.
		+	You may change the PDB parameter (which sets the PDB file loaded into the applet)
		+	or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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		+	{{STRUCTURE_3ztx\| PDB=3ztx \| SCENE= }}

-	~~Authors: Kwiatkowski, N., Villa, F., Musacchio, A., Gray, N~~.	+	===Aurora kinase selective inhibitors identified using a Taxol-induced checkpoint sensitivity screen.===

-	~~Description~~: ~~Aurora kinase selective inhibitors identified using~~ a Taxol-induced checkpoint ~~sensitivity screen.~~	+
		+	<!--
		+	The line below this paragraph, {{ABSTRACT_PUBMED_21992004}}, adds the Publication Abstract to the page
		+	(as it appears on PubMed at http://www.pubmed.gov), where 21992004 is the PubMed ID number.
		+	-->
		+	{{ABSTRACT_PUBMED_21992004}}
		+
		+	==About this Structure==
		+	[[3ztx]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Xenopus_laevis Xenopus laevis]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3ZTX OCA].
		+
		+	==Reference==
		+	<ref group="xtra">PMID:021992004</ref><references group="xtra"/>
		+	[[Category: Non-specific serine/threonine protein kinase]]
		+	[[Category: Xenopus laevis]]
		+	[[Category: Gray, N.]]
		+	[[Category: Kwiatkowski, N.]]
		+	[[Category: Musacchio, A.]]
		+	[[Category: Villa, F.]]
		+	[[Category: Taxol-induced checkpoint inhibitor]]
		+	[[Category: Transferase]]
		+	[[Category: Transferase-cell cycle complex]]

OCA: Protected "3ztx" [edit=sysop:move=sysop]

OCA — Wed, 20 Jul 2011 06:21:57 GMT

Protected "3ztx" [edit=sysop:move=sysop]

←Older revision

Revision as of 06:21, 20 July 2011

OCA: New page: '''Unreleased structure''' The entry 3ztx is ON HOLD until Paper Publication Authors: Kwiatkowski, N., Villa, F., Musacchio, A., Gray, N. Description: Aurora kinase selective inhibitor...

OCA — Wed, 20 Jul 2011 06:21:56 GMT

New page: '''Unreleased structure''' The entry 3ztx is ON HOLD until Paper Publication Authors: Kwiatkowski, N., Villa, F., Musacchio, A., Gray, N. Description: Aurora kinase selective inhibitor...

New page

'''Unreleased structure'''

The entry 3ztx is ON HOLD until Paper Publication

Authors: Kwiatkowski, N., Villa, F., Musacchio, A., Gray, N.

Description: Aurora kinase selective inhibitors identified using a Taxol-induced checkpoint sensitivity screen.

←Older revision		Revision as of 07:17, 18 August 2022
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	<StructureSection load='3ztx' size='340' side='right'caption='[[3ztx]], [[Resolution\|resolution]] 1.95Å' scene=''>		<StructureSection load='3ztx' size='340' side='right'caption='[[3ztx]], [[Resolution\|resolution]] 1.95Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[3ztx]] is a 4 chain structure with sequence from [~~http~~://en.wikipedia.org/wiki/African_clawed_frog African clawed frog]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3ZTX OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://proteopedia.org/fgij/fg.htm?mol=3ZTX FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[3ztx]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/African_clawed_frog African clawed frog]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3ZTX OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3ZTX FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ZTX:2-((4-(4-HYDROXYPIPERIDIN-1-YL)PHENYL)AMINO)-5,11-DIMETHYL-5H-BENZO[E]PYRIMIDO+[5,4-B][1,4]DIAZEPIN-6(11H)-ONE'>ZTX</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ZTX:2-((4-(4-HYDROXYPIPERIDIN-1-YL)PHENYL)AMINO)-5,11-DIMETHYL-5H-BENZO[E]PYRIMIDO+[5,4-B][1,4]DIAZEPIN-6(11H)-ONE'>ZTX</scene></td></tr>
	<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene></td></tr>		<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene></td></tr>
-	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[2bfx\|2bfx]], [[2vgo\|2vgo]], [[2vrx\|2vrx]], [[2vgp\|2vgp]], [[2bfy\|2bfy]]</td></tr>	+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[2bfx\|2bfx]], [[2vgo\|2vgo]], [[2vrx\|2vrx]], [[2vgp\|2vgp]], [[2bfy\|2bfy]]</div></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'>[https://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [https://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~~://proteopedia.org/fgij/fg.htm?mol=3ztx FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3ztx OCA], [~~http~~://pdbe.org/3ztx PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=3ztx RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/3ztx PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=3ztx ProSAT]</span></td></tr>	+	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=3ztx FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3ztx OCA], [https://pdbe.org/3ztx PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3ztx RCSB], [https://www.ebi.ac.uk/pdbsum/3ztx PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3ztx ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[[~~http~~://www.uniprot.org/uniprot/AUKBA_XENLA AUKBA_XENLA]] Serine/threonine-protein kinase component of the chromosomal passenger complex (CPC), a complex that acts as a key regulator of mitosis. The CPC complex has essential functions at the centromere in ensuring correct chromosome alignment and segregation and is required for chromatin-induced microtubule stabilization and spindle assembly. Involved in the bipolar attachment of spindle microtubules to kinetochores and is a key regulator for the onset of cytokinesis during mitosis. Required for central/midzone spindle assembly and cleavage furrow formation. Phosphorylates 'Ser-10' of histone H3 during mitosis.<ref>PMID:12221116</ref> <ref>PMID:11350965</ref> <ref>PMID:17199039</ref> [[~~http~~://www.uniprot.org/uniprot/INCEA_XENLA INCEA_XENLA]] Component of the chromosomal passenger complex (CPC), a complex that acts as a key regulator of mitosis. The CPC complex has essential functions at the centromere in ensuring correct chromosome alignment and segregation and is required for chromatin-induced microtubule stabilization and spindle assembly. Probably acts through association with aurkb or aurkc. Seems to bind directly to microtubules.<ref>PMID:12221116</ref> <ref>PMID:17199039</ref>	+	[[https://www.uniprot.org/uniprot/AUKBA_XENLA AUKBA_XENLA]] Serine/threonine-protein kinase component of the chromosomal passenger complex (CPC), a complex that acts as a key regulator of mitosis. The CPC complex has essential functions at the centromere in ensuring correct chromosome alignment and segregation and is required for chromatin-induced microtubule stabilization and spindle assembly. Involved in the bipolar attachment of spindle microtubules to kinetochores and is a key regulator for the onset of cytokinesis during mitosis. Required for central/midzone spindle assembly and cleavage furrow formation. Phosphorylates 'Ser-10' of histone H3 during mitosis.<ref>PMID:12221116</ref> <ref>PMID:11350965</ref> <ref>PMID:17199039</ref> [[https://www.uniprot.org/uniprot/INCEA_XENLA INCEA_XENLA]] Component of the chromosomal passenger complex (CPC), a complex that acts as a key regulator of mitosis. The CPC complex has essential functions at the centromere in ensuring correct chromosome alignment and segregation and is required for chromatin-induced microtubule stabilization and spindle assembly. Probably acts through association with aurkb or aurkc. Seems to bind directly to microtubules.<ref>PMID:12221116</ref> <ref>PMID:17199039</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==