1sqo - Revision history

OCA at 08:34, 1 May 2024

OCA — Wed, 01 May 2024 08:34:20 GMT

←Older revision		Revision as of 08:34, 1 May 2024
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	<StructureSection load='1sqo' size='340' side='right'caption='[[1sqo]], [[Resolution\|resolution]] 1.84Å' scene=''>		<StructureSection load='1sqo' size='340' side='right'caption='[[1sqo]], [[Resolution\|resolution]] 1.84Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[1sqo]] 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=1SQO OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://proteopedia.org/fgij/fg.htm?mol=1SQO FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[1sqo]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1SQO OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1SQO FirstGlance]. <br>
-	</td></tr><tr id='~~ligand~~'><td class="sblockLbl"><b>[[~~Ligand~~\|~~Ligands~~:]]</b></td><td class="sblockDat" id="~~ligandDat~~">~~<scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>~~, ~~<scene name='pdbligand=UI2:8-(PYRIMIDIN-2-YLAMINO)NAPHTHALENE-2-CARBOXIMIDAMIDE'>UI2</scene></td></tr>~~	+	</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models\|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution\|Resolution]] 1.84Å</td></tr>
-	~~<tr id='related'><td class="sblockLbl"><b>~~[[~~Related_structure~~\|~~Related:~~]]~~</b></td><td class="sblockDat"><div style='overflow: auto~~; ~~max-height: 3em;'>[[1owd\|1owd]], [[1owe\|1owe]], [[1owh\|1owh]], [[1owi\|1owi]], [[1owj\|1owj]], [[1owk\|1owk]], [[1sqa\|1sqa]], [[1sqt\|1sqt]]</div>~~</td></tr>	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=UI2:8-(PYRIMIDIN-2-YLAMINO)NAPHTHALENE-2-CARBOXIMIDAMIDE'>UI2</scene></td></tr>
-	<tr id='~~gene~~'><td class="sblockLbl"><b>[[~~Gene~~\|~~Gene~~:]]</b></td><td class="sblockDat"~~>PLAU ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&~~id=~~9606 HUMAN])</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=1sqo FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1sqo OCA], [https://pdbe.org/1sqo PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1sqo RCSB], [https://www.ebi.ac.uk/pdbsum/1sqo PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1sqo ProSAT]</span></td></tr>
-	~~<tr id~~='~~activity'><td class~~=~~"sblockLbl"><b>Activity~~:~~</b~~></td><~~td class~~=~~"sblockDat"><span class~~=~~'plainlinks'>[http~~:~~//en.wikipedia.org/wiki/U~~-~~plasminogen_activator U~~-~~plasminogen activator], with EC number [http://www.brenda~~-~~enzymes.info/php/result_flat.php4?ecno=3.4.21.73 3.4.21.73]~~ </~~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=1sqo FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1sqo OCA], [~~http~~://pdbe.org/1sqo PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=1sqo RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/1sqo PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=1sqo ProSAT]</span></td></tr>	+
	</table>		</table>
	== Disease ==		== Disease ==
-	[~~[http~~://www.uniprot.org/uniprot/UROK_HUMAN UROK_HUMAN]] Defects in PLAU are the cause of Quebec platelet disorder (QPD) [MIM:[~~http~~://omim.org/entry/601709 601709]]. QPD is an autosomal dominant bleeding disorder due to a gain-of-function defect in fibrinolysis. Although affected individuals do not exhibit systemic fibrinolysis, they show delayed onset bleeding after challenge, such as surgery. The hallmark of the disorder is markedly increased PLAU levels within platelets, which causes intraplatelet plasmin generation and secondary degradation of alpha-granule proteins.<ref>PMID:20007542</ref>	+	[https://www.uniprot.org/uniprot/UROK_HUMAN UROK_HUMAN] Defects in PLAU are the cause of Quebec platelet disorder (QPD) [MIM:[https://omim.org/entry/601709 601709]. QPD is an autosomal dominant bleeding disorder due to a gain-of-function defect in fibrinolysis. Although affected individuals do not exhibit systemic fibrinolysis, they show delayed onset bleeding after challenge, such as surgery. The hallmark of the disorder is markedly increased PLAU levels within platelets, which causes intraplatelet plasmin generation and secondary degradation of alpha-granule proteins.<ref>PMID:20007542</ref>
	== Function ==		== Function ==
-	[~~[http~~://www.uniprot.org/uniprot/UROK_HUMAN UROK_HUMAN]] Specifically cleaves the zymogen plasminogen to form the active enzyme plasmin.	+	[https://www.uniprot.org/uniprot/UROK_HUMAN UROK_HUMAN] Specifically cleaves the zymogen plasminogen to form the active enzyme plasmin.
	== Evolutionary Conservation ==		== Evolutionary Conservation ==
	[[Image:Consurf_key_small.gif\|200px\|right]]		[[Image:Consurf_key_small.gif\|200px\|right]]
Line 24:		Line 22:
	</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary\|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=1sqo ConSurf].		</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary\|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=1sqo ConSurf].
	<div style="clear:both"></div>		<div style="clear:both"></div>
-	<div style="background-color:#fffaf0;">
-	== Publication Abstract from PubMed ==
-	Several 8-substituted 2-naphthamidine-based inhibitors of the serine protease urokinase plasminogen activator (uPA) are described. Direct attachment of five-membered saturated or unsaturated rings improved inhibitor performance; substitution with sulfones further improved binding profiles. Combination of these substituents or of previously described NH-linked heteroaromatic rings with 6-phenyl amide substituents provided further enhancements to potency and selectivity.
-
-	Interaction with the S1 beta-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors.,Wendt MD, Geyer A, McClellan WJ, Rockway TW, Weitzberg M, Zhao X, Mantei R, Stewart K, Nienaber V, Klinghofer V, Giranda VL Bioorg Med Chem Lett. 2004 Jun 21;14(12):3063-8. PMID:15149645<ref>PMID:15149645</ref>
-
-	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	</div>
-	<div class="pdbe-citations 1sqo" style="background-color:#fffaf0;"></div>

	==See Also==		==See Also==
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	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Human~~]]	+	[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	~~[[Category: U-plasminogen activator]]~~	+	[[Category: Geyer A]]
-	[[Category: Geyer, A]]	+	[[Category: Giranda VL]]
-	[[Category: Giranda~~, V L~~]]	+	[[Category: Klinghofer V]]
-	[[Category: Klinghofer, V]]	+	[[Category: Mantei R]]
-	[[Category: Mantei, R]]	+	[[Category: McClellan WJ]]
-	[[Category: McClellan~~, W J~~]]	+	[[Category: Nienaber V]]
-	[[Category: Nienaber, V]]	+	[[Category: Rockway TW]]
-	[[Category: Rockway~~, T W~~]]	+	[[Category: Stewart K]]
-	[[Category: Stewart, K]]	+	[[Category: Weitzberg M]]
-	[[Category: Weitzberg, M]]	+	[[Category: Wendt MD]]
-	[[Category: Wendt~~, M D~~]]	+	[[Category: Zhao X]]
-	[[Category: Zhao, X]]	+
-	~~[[Category: Egf-like domain]]~~	+
-	~~[[Category: Glycoprotein]]~~	+
-	~~[[Category: Hydrolase]]~~	+
-	~~[[Category: Kringle]]~~	+
-	~~[[Category: Plasminogen activation]]~~	+
-	~~[[Category: Serine protease~~]]	+

OCA at 11:32, 24 December 2020

OCA — Thu, 24 Dec 2020 11:32:24 GMT

←Older revision		Revision as of 11:32, 24 December 2020
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	==Substituted 2-Naphthamidine Inhibitors of Urokinase==		==Substituted 2-Naphthamidine Inhibitors of Urokinase==
-	<StructureSection load='1sqo' size='340' side='right' caption='[[1sqo]], [[Resolution\|resolution]] 1.84Å' scene=''>	+	<StructureSection load='1sqo' size='340' side='right'caption='[[1sqo]], [[Resolution\|resolution]] 1.84Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[1sqo]] 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=1SQO OCA]. For a <b>guided tour on the structure components</b> use [http://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=1SQO FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[1sqo]] 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=1SQO OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=1SQO FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=UI2:8-(PYRIMIDIN-2-YLAMINO)NAPHTHALENE-2-CARBOXIMIDAMIDE'>UI2</scene></td></tr>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=UI2:8-(PYRIMIDIN-2-YLAMINO)NAPHTHALENE-2-CARBOXIMIDAMIDE'>UI2</scene></td></tr>
-	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1owd\|1owd]], [[1owe\|1owe]], [[1owh\|1owh]], [[1owi\|1owi]], [[1owj\|1owj]], [[1owk\|1owk]], [[1sqa\|1sqa]], [[1sqt\|1sqt]]</td></tr>	+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[1owd\|1owd]], [[1owe\|1owe]], [[1owh\|1owh]], [[1owi\|1owi]], [[1owj\|1owj]], [[1owk\|1owk]], [[1sqa\|1sqa]], [[1sqt\|1sqt]]</div></td></tr>
	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">PLAU ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>		<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">PLAU ([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/U-plasminogen_activator U-plasminogen activator], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.73 3.4.21.73] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/U-plasminogen_activator U-plasminogen activator], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.73 3.4.21.73] </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=1sqo FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1sqo OCA], [http://pdbe.org/1sqo PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=1sqo RCSB], [http://www.ebi.ac.uk/pdbsum/1sqo PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=1sqo 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=1sqo FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1sqo OCA], [http://pdbe.org/1sqo PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=1sqo RCSB], [http://www.ebi.ac.uk/pdbsum/1sqo PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=1sqo ProSAT]</span></td></tr>
	</table>		</table>
	== Disease ==		== Disease ==
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	==See Also==		==See Also==
-	*[[Urokinase\|Urokinase]]	+	*[[Urokinase 3D Structures\|Urokinase 3D Structures]]
	== References ==		== References ==
	<references/>		<references/>
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	</StructureSection>		</StructureSection>
	[[Category: Human]]		[[Category: Human]]
		+	[[Category: Large Structures]]
	[[Category: U-plasminogen activator]]		[[Category: U-plasminogen activator]]
	[[Category: Geyer, A]]		[[Category: Geyer, A]]

OCA at 07:58, 14 March 2018

OCA — Wed, 14 Mar 2018 07:58:17 GMT

←Older revision		Revision as of 07:58, 14 March 2018
Line 1:		Line 1:
		+
	==Substituted 2-Naphthamidine Inhibitors of Urokinase==		==Substituted 2-Naphthamidine Inhibitors of Urokinase==
	<StructureSection load='1sqo' size='340' side='right' caption='[[1sqo]], [[Resolution\|resolution]] 1.84Å' scene=''>		<StructureSection load='1sqo' size='340' side='right' caption='[[1sqo]], [[Resolution\|resolution]] 1.84Å' scene=''>
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	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">PLAU ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>		<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">PLAU ([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/U-plasminogen_activator U-plasminogen activator], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.73 3.4.21.73] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/U-plasminogen_activator U-plasminogen activator], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.73 3.4.21.73] </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=1sqo FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1sqo OCA], [http://pdbe.org/1sqo PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=1sqo RCSB], [http://www.ebi.ac.uk/pdbsum/1sqo 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=1sqo FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1sqo OCA], [http://pdbe.org/1sqo PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=1sqo RCSB], [http://www.ebi.ac.uk/pdbsum/1sqo PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=1sqo ProSAT]</span></td></tr>
	</table>		</table>
	== Disease ==		== Disease ==
Line 17:		Line 18:
	Check<jmol>		Check<jmol>
	<jmolCheckbox>		<jmolCheckbox>
-	<scriptWhenChecked>select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/sq/1sqo_consurf.spt"</scriptWhenChecked>	+	<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/sq/1sqo_consurf.spt"</scriptWhenChecked>
	<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>		<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
	<text>to colour the structure by Evolutionary Conservation</text>		<text>to colour the structure by Evolutionary Conservation</text>
	</jmolCheckbox>		</jmolCheckbox>
-	</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary\|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/~~chain_selection~~.php?pdb_ID=~~2ata~~ ConSurf].	+	</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary\|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=1sqo ConSurf].
	<div style="clear:both"></div>		<div style="clear:both"></div>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">

OCA at 02:34, 12 September 2015

OCA — Sat, 12 Sep 2015 02:34:37 GMT

←Older revision		Revision as of 02:34, 12 September 2015
Line 2:		Line 2:
	<StructureSection load='1sqo' size='340' side='right' caption='[[1sqo]], [[Resolution\|resolution]] 1.84Å' scene=''>		<StructureSection load='1sqo' size='340' side='right' caption='[[1sqo]], [[Resolution\|resolution]] 1.84Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[1sqo]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/~~Homo_sapiens Homo sapiens~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1SQO OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1SQO FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[1sqo]] 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=1SQO OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1SQO FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=UI2:8-(PYRIMIDIN-2-YLAMINO)NAPHTHALENE-2-CARBOXIMIDAMIDE'>UI2</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=UI2:8-(PYRIMIDIN-2-YLAMINO)NAPHTHALENE-2-CARBOXIMIDAMIDE'>UI2</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1owd\|1owd]], [[1owe\|1owe]], [[1owh\|1owh]], [[1owi\|1owi]], [[1owj\|1owj]], [[1owk\|1owk]], [[1sqa\|1sqa]], [[1sqt\|1sqt]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1owd\|1owd]], [[1owe\|1owe]], [[1owh\|1owh]], [[1owi\|1owi]], [[1owj\|1owj]], [[1owk\|1owk]], [[1sqa\|1sqa]], [[1sqt\|1sqt]]</td></tr>
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">PLAU ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 ~~Homo sapiens~~])</td></tr>	+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">PLAU ([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/U-plasminogen_activator U-plasminogen activator], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.73 3.4.21.73] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/U-plasminogen_activator U-plasminogen activator], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.73 3.4.21.73] </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=1sqo FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1sqo OCA], [http://www.rcsb.org/pdb/explore.do?structureId=1sqo RCSB], [http://www.ebi.ac.uk/pdbsum/1sqo 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=1sqo FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1sqo OCA], [http://pdbe.org/1sqo PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=1sqo RCSB], [http://www.ebi.ac.uk/pdbsum/1sqo PDBsum]</span></td></tr>
	</table>		</table>
	== Disease ==		== Disease ==
Line 31:		Line 31:
	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 1sqo" style="background-color:#fffaf0;"></div>

	==See Also==		==See Also==
Line 38:		Line 39:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Homo sapiens~~]]	+	[[Category: Human]]
	[[Category: U-plasminogen activator]]		[[Category: U-plasminogen activator]]
	[[Category: Geyer, A]]		[[Category: Geyer, A]]

OCA at 08:20, 6 January 2015

OCA — Tue, 06 Jan 2015 08:20:55 GMT

←Older revision		Revision as of 08:20, 6 January 2015
Line 3:		Line 3:
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[1sqo]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1SQO OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1SQO FirstGlance]. <br>		<table><tr><td colspan='2'>[[1sqo]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1SQO OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1SQO FirstGlance]. <br>
-	</td></tr><tr><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=UI2:8-(PYRIMIDIN-2-YLAMINO)NAPHTHALENE-2-CARBOXIMIDAMIDE'>UI2</scene><br>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=UI2:8-(PYRIMIDIN-2-YLAMINO)NAPHTHALENE-2-CARBOXIMIDAMIDE'>UI2</scene></td></tr>
-	<tr><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1owd\|1owd]], [[1owe\|1owe]], [[1owh\|1owh]], [[1owi\|1owi]], [[1owj\|1owj]], [[1owk\|1owk]], [[1sqa\|1sqa]], [[1sqt\|1sqt]]</td></tr>	+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1owd\|1owd]], [[1owe\|1owe]], [[1owh\|1owh]], [[1owi\|1owi]], [[1owj\|1owj]], [[1owk\|1owk]], [[1sqa\|1sqa]], [[1sqt\|1sqt]]</td></tr>
-	<tr><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">PLAU ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</td></tr>	+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">PLAU ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</td></tr>
-	<tr><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/U-plasminogen_activator U-plasminogen activator], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.73 3.4.21.73] </span></td></tr>	+	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/U-plasminogen_activator U-plasminogen activator], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.73 3.4.21.73] </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=1sqo FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1sqo OCA], [http://www.rcsb.org/pdb/explore.do?structureId=1sqo RCSB], [http://www.ebi.ac.uk/pdbsum/1sqo 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=1sqo FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1sqo OCA], [http://www.rcsb.org/pdb/explore.do?structureId=1sqo RCSB], [http://www.ebi.ac.uk/pdbsum/1sqo PDBsum]</span></td></tr>
-	<table>	+	</table>
	== Disease ==		== Disease ==
	[[http://www.uniprot.org/uniprot/UROK_HUMAN UROK_HUMAN]] Defects in PLAU are the cause of Quebec platelet disorder (QPD) [MIM:[http://omim.org/entry/601709 601709]]. QPD is an autosomal dominant bleeding disorder due to a gain-of-function defect in fibrinolysis. Although affected individuals do not exhibit systemic fibrinolysis, they show delayed onset bleeding after challenge, such as surgery. The hallmark of the disorder is markedly increased PLAU levels within platelets, which causes intraplatelet plasmin generation and secondary degradation of alpha-granule proteins.<ref>PMID:20007542</ref>		[[http://www.uniprot.org/uniprot/UROK_HUMAN UROK_HUMAN]] Defects in PLAU are the cause of Quebec platelet disorder (QPD) [MIM:[http://omim.org/entry/601709 601709]]. QPD is an autosomal dominant bleeding disorder due to a gain-of-function defect in fibrinolysis. Although affected individuals do not exhibit systemic fibrinolysis, they show delayed onset bleeding after challenge, such as surgery. The hallmark of the disorder is markedly increased PLAU levels within platelets, which causes intraplatelet plasmin generation and secondary degradation of alpha-granule proteins.<ref>PMID:20007542</ref>
Line 40:		Line 40:
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
	[[Category: U-plasminogen activator]]		[[Category: U-plasminogen activator]]
-	[[Category: Geyer, A.]]	+	[[Category: Geyer, A]]
-	[[Category: Giranda, V L.]]	+	[[Category: Giranda, V L]]
-	[[Category: Klinghofer, V.]]	+	[[Category: Klinghofer, V]]
-	[[Category: Mantei, R.]]	+	[[Category: Mantei, R]]
-	[[Category: McClellan, W J.]]	+	[[Category: McClellan, W J]]
-	[[Category: Nienaber, V.]]	+	[[Category: Nienaber, V]]
-	[[Category: Rockway, T W.]]	+	[[Category: Rockway, T W]]
-	[[Category: Stewart, K.]]	+	[[Category: Stewart, K]]
-	[[Category: Weitzberg, M.]]	+	[[Category: Weitzberg, M]]
-	[[Category: Wendt, M D.]]	+	[[Category: Wendt, M D]]
-	[[Category: Zhao, X.]]	+	[[Category: Zhao, X]]
	[[Category: Egf-like domain]]		[[Category: Egf-like domain]]
	[[Category: Glycoprotein]]		[[Category: Glycoprotein]]

OCA at 17:34, 29 September 2014

OCA — Mon, 29 Sep 2014 17:34:42 GMT

←Older revision		Revision as of 17:34, 29 September 2014
Line 1:		Line 1:
-	~~{{STRUCTURE_1sqo\| PDB~~=1sqo \| ~~SCENE~~= }}	+	==Substituted 2-Naphthamidine Inhibitors of Urokinase==
-	===~~Substituted~~ 2-~~Naphthamidine Inhibitors~~ of ~~Urokinase~~===	+	<StructureSection load='1sqo' size='340' side='right' caption='[[1sqo]], [[Resolution\|resolution]] 1.84Å' scene=''>
-	~~{{ABSTRACT_PUBMED_15149645}}~~	+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[1sqo]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1SQO OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1SQO FirstGlance]. <br>
		+	</td></tr><tr><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=UI2:8-(PYRIMIDIN-2-YLAMINO)NAPHTHALENE-2-CARBOXIMIDAMIDE'>UI2</scene><br>
		+	<tr><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1owd\|1owd]], [[1owe\|1owe]], [[1owh\|1owh]], [[1owi\|1owi]], [[1owj\|1owj]], [[1owk\|1owk]], [[1sqa\|1sqa]], [[1sqt\|1sqt]]</td></tr>
		+	<tr><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">PLAU ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</td></tr>
		+	<tr><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/U-plasminogen_activator U-plasminogen activator], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.73 3.4.21.73] </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=1sqo FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1sqo OCA], [http://www.rcsb.org/pdb/explore.do?structureId=1sqo RCSB], [http://www.ebi.ac.uk/pdbsum/1sqo PDBsum]</span></td></tr>
		+	<table>
		+	== Disease ==
		+	[[http://www.uniprot.org/uniprot/UROK_HUMAN UROK_HUMAN]] Defects in PLAU are the cause of Quebec platelet disorder (QPD) [MIM:[http://omim.org/entry/601709 601709]]. QPD is an autosomal dominant bleeding disorder due to a gain-of-function defect in fibrinolysis. Although affected individuals do not exhibit systemic fibrinolysis, they show delayed onset bleeding after challenge, such as surgery. The hallmark of the disorder is markedly increased PLAU levels within platelets, which causes intraplatelet plasmin generation and secondary degradation of alpha-granule proteins.<ref>PMID:20007542</ref>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/UROK_HUMAN UROK_HUMAN]] Specifically cleaves the zymogen plasminogen to form the active enzyme plasmin.
		+	== Evolutionary Conservation ==
		+	[[Image:Consurf_key_small.gif\|200px\|right]]
		+	Check<jmol>
		+	<jmolCheckbox>
		+	<scriptWhenChecked>select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/sq/1sqo_consurf.spt"</scriptWhenChecked>
		+	<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
		+	<text>to colour the structure by Evolutionary Conservation</text>
		+	</jmolCheckbox>
		+	</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary\|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/chain_selection.php?pdb_ID=2ata ConSurf].
		+	<div style="clear:both"></div>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Several 8-substituted 2-naphthamidine-based inhibitors of the serine protease urokinase plasminogen activator (uPA) are described. Direct attachment of five-membered saturated or unsaturated rings improved inhibitor performance; substitution with sulfones further improved binding profiles. Combination of these substituents or of previously described NH-linked heteroaromatic rings with 6-phenyl amide substituents provided further enhancements to potency and selectivity.

-	~~==Disease==~~	+	Interaction with the S1 beta-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors.,Wendt MD, Geyer A, McClellan WJ, Rockway TW, Weitzberg M, Zhao X, Mantei R, Stewart K, Nienaber V, Klinghofer V, Giranda VL Bioorg Med Chem Lett. 2004 Jun 21;14(12):3063-8. PMID:15149645<ref>PMID:15149645</ref>
-	~~[[http://www.uniprot.org/uniprot/UROK_HUMAN UROK_HUMAN]] Defects in PLAU are~~ the ~~cause~~ of ~~Quebec platelet disorder (QPD) [MIM~~:~~[http://omim.org/entry/601709 601709]]. QPD is an autosomal dominant bleeding disorder due to a gain~~-of-~~function defect in fibrinolysis~~. ~~Although affected individuals do not exhibit systemic fibrinolysis~~, ~~they show delayed onset bleeding after challenge~~, ~~such as surgery. The hallmark of the disorder is markedly increased PLAU levels within platelets~~, ~~which causes intraplatelet plasmin generation and secondary degradation of alpha~~-~~granule proteins~~.<ref>PMID:~~20007542~~</ref>	+

-	~~==Function==~~	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	~~[[http:~~/~~/www~~.~~uniprot~~.~~org/uniprot/UROK_HUMAN UROK_HUMAN]] Specifically cleaves the zymogen plasminogen to form the active enzyme plasmin~~.	+	</div>
-		+
-	~~==About this Structure==~~	+
-	~~[[1sqo]] is a 1 chain structure with sequence from [http:~~/~~/en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1SQO OCA].~~	+

	==See Also==		==See Also==
	*[[Urokinase\|Urokinase]]		*[[Urokinase\|Urokinase]]
-		+	== References ==
-	==~~Reference~~==	+	<references/>
-	~~<ref group="xtra">PMID:015149645</ref>~~<references ~~group="xtra"~~/><~~references~~/>	+	__TOC__
		+	</StructureSection>
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
	[[Category: U-plasminogen activator]]		[[Category: U-plasminogen activator]]

OCA at 07:09, 25 March 2013

OCA — Mon, 25 Mar 2013 07:09:33 GMT

←Older revision		Revision as of 07:09, 25 March 2013
Line 1:		Line 1:
-	[[Image:1sqo.png\|left\|200px]]
-
	{{STRUCTURE_1sqo\| PDB=1sqo \| SCENE= }}		{{STRUCTURE_1sqo\| PDB=1sqo \| SCENE= }}
-
	===Substituted 2-Naphthamidine Inhibitors of Urokinase===		===Substituted 2-Naphthamidine Inhibitors of Urokinase===
		+	{{ABSTRACT_PUBMED_15149645}}

-	~~{{ABSTRACT_PUBMED_15149645}}~~	+	==Disease==
		+	[[http://www.uniprot.org/uniprot/UROK_HUMAN UROK_HUMAN]] Defects in PLAU are the cause of Quebec platelet disorder (QPD) [MIM:[http://omim.org/entry/601709 601709]]. QPD is an autosomal dominant bleeding disorder due to a gain-of-function defect in fibrinolysis. Although affected individuals do not exhibit systemic fibrinolysis, they show delayed onset bleeding after challenge, such as surgery. The hallmark of the disorder is markedly increased PLAU levels within platelets, which causes intraplatelet plasmin generation and secondary degradation of alpha-granule proteins.<ref>PMID:20007542</ref>
		+
		+	==Function==
		+	[[http://www.uniprot.org/uniprot/UROK_HUMAN UROK_HUMAN]] Specifically cleaves the zymogen plasminogen to form the active enzyme plasmin.

	==About this Structure==		==About this Structure==
Line 14:		Line 16:

	==Reference==		==Reference==
-	<ref group="xtra">PMID:015149645</ref><references group="xtra"/>	+	<ref group="xtra">PMID:015149645</ref><references group="xtra"/><references/>
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
	[[Category: U-plasminogen activator]]		[[Category: U-plasminogen activator]]

OCA at 22:33, 20 October 2012

OCA — Sat, 20 Oct 2012 22:33:27 GMT

←Older revision		Revision as of 22:33, 20 October 2012
Line 8:		Line 8:

	==About this Structure==		==About this Structure==
-	[[1sqo]] is a 1 chain structure ~~of [[Urokinase]]~~ with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1SQO OCA].	+	[[1sqo]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1SQO OCA].

	==See Also==		==See Also==

OCA: Protected "1sqo" [edit=sysop:move=sysop]

OCA — Fri, 27 Jul 2012 16:43:12 GMT

Protected "1sqo" [edit=sysop:move=sysop]

←Older revision

Revision as of 16:43, 27 July 2012

OCA at 16:43, 27 July 2012

OCA — Fri, 27 Jul 2012 16:43:11 GMT

←Older revision		Revision as of 16:43, 27 July 2012
Line 1:		Line 1:
-	{{Seed}}
	[[Image:1sqo.png\|left\|200px]]		[[Image:1sqo.png\|left\|200px]]

-	<!--
-	The line below this paragraph, containing "STRUCTURE_1sqo", 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),
-	or leave the SCENE parameter empty for the default display.
-	-->
	{{STRUCTURE_1sqo\| PDB=1sqo \| SCENE= }}		{{STRUCTURE_1sqo\| PDB=1sqo \| SCENE= }}

	===Substituted 2-Naphthamidine Inhibitors of Urokinase===		===Substituted 2-Naphthamidine Inhibitors of Urokinase===

-
-	<!--
-	The line below this paragraph, {{ABSTRACT_PUBMED_15149645}}, adds the Publication Abstract to the page
-	(as it appears on PubMed at http://www.pubmed.gov), where 15149645 is the PubMed ID number.
-	-->
	{{ABSTRACT_PUBMED_15149645}}		{{ABSTRACT_PUBMED_15149645}}
-
-	==Disease==
-	Known disease associated with this structure: Alzheimer disease, late-onset, susceptibility to OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=191840 191840]]

	==About this Structure==		==About this Structure==
-	~~1SQO~~ is a 1 chain structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1SQO OCA].	+	[[1sqo]] is a 1 chain structure of [[Urokinase]] with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1SQO OCA].
		+
		+	==See Also==
		+	*[[Urokinase\|Urokinase]]

	==Reference==		==Reference==
-	<ref group="xtra">PMID:~~15149645~~</ref><references group="xtra"/>	+	<ref group="xtra">PMID:015149645</ref><references group="xtra"/>
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
	[[Category: U-plasminogen activator]]		[[Category: U-plasminogen activator]]
Line 46:		Line 34:
	[[Category: Plasminogen activation]]		[[Category: Plasminogen activation]]
	[[Category: Serine protease]]		[[Category: Serine protease]]
-
-	''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Feb 18 10:06:15 2009''