3qup - Revision history

OCA at 10:50, 21 February 2024

2024-02-21T10:50:10Z

←Older revision		Revision as of 10:50, 21 February 2024
Line 3:		Line 3:
	<StructureSection load='3qup' size='340' side='right'caption='[[3qup]], [[Resolution\|resolution]] 1.90Å' scene=''>		<StructureSection load='3qup' size='340' side='right'caption='[[3qup]], [[Resolution\|resolution]] 1.90Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[3qup]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/~~Lk3_transgenic_mice Lk3 transgenic mice~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3QUP OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3QUP FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[3qup]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Mus_musculus Mus musculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3QUP OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3QUP FirstGlance]. <br>
-	</td></tr><tr id='~~ligand~~'><td class="sblockLbl"><b>[[~~Ligand~~\|~~Ligands~~:]]</b></td><td class="sblockDat" id="~~ligandDat~~">~~<scene name='pdbligand=LUN:(5~~-~~FLUORO-1H-INDOL-2-YL)~~[~~(3R)-1-~~[~~(3R)-PIPERIDIN-3-YL~~]~~SPIRO[INDOLE-3,3-PYRROLIDIN~~]-1~~(2H)-YL]METHANONE'>LUN</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]] 1.9Å</td></tr>
-	<tr id='~~gene~~'><td class="sblockLbl"><b>[[~~Gene~~\|~~Gene~~:]]</b></td><td class="sblockDat"~~>Tyro3, Dtk, Rse ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&~~id~~=10090 LK3 transgenic mice])</td></tr>~~	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=LUN:(5-FLUORO-1H-INDOL-2-YL)[(3R)-1-[(3R)-PIPERIDIN-3-YL]SPIRO[INDOLE-3,3-PYRROLIDIN]-1(2H)-YL]METHANONE'>LUN</scene></td></tr>
-	~~<tr id='activity'><td class~~="~~sblockLbl~~"><~~b>Activity:</b></td><td class~~=~~"sblockDat"><span class~~=~~'plainlinks'>[https~~:~~//en.wikipedia.org/wiki/Receptor_protein~~-~~tyrosine_kinase Receptor protein~~-~~tyrosine kinase~~]~~, with EC number~~ [~~https://www.brenda~~-~~enzymes.info/php/result_flat.php4?ecno=2.7.10.1 2.7.10.~~1] </~~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=3qup FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3qup OCA], [https://pdbe.org/3qup PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3qup RCSB], [https://www.ebi.ac.uk/pdbsum/3qup PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3qup 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=3qup FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3qup OCA], [https://pdbe.org/3qup PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3qup RCSB], [https://www.ebi.ac.uk/pdbsum/3qup PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3qup ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[[https://www.uniprot.org/uniprot/TYRO3_MOUSE TYRO3_MOUSE]] Receptor tyrosine kinase that transduces signals from the extracellular matrix into the cytoplasm by binding to several ligands including TULP1 or GAS6. Regulates many physiological processes including cell survival, migration and differentiation. Ligand binding at the cell surface induces dimerization and autophosphorylation of TYRO3 on its intracellular domain that provides docking sites for downstream signaling molecules. Following activation by ligand, interacts with PIK3R1 and thereby enhances PI3-kinase activity. Activates the AKT survival pathway, including nuclear translocation of NF-kappa-B and up-regulation of transcription of NF-kappa-B-regulated genes. TYRO3 signaling plays a role in various processes such as neuron protection from excitotoxic injury, platelet aggregation and cytoskeleton reorganization. Plays also an important role in inhibition of Toll-like receptors (TLRs)-mediated innate immune response by activating STAT1, which selectively induces production of suppressors of cytokine signaling SOCS1 and SOCS3.<ref>PMID:15650770</ref> <ref>PMID:20363878</ref> <ref>PMID:21084607</ref> <ref>PMID:21291561</ref>	+	[https://www.uniprot.org/uniprot/TYRO3_MOUSE TYRO3_MOUSE] Receptor tyrosine kinase that transduces signals from the extracellular matrix into the cytoplasm by binding to several ligands including TULP1 or GAS6. Regulates many physiological processes including cell survival, migration and differentiation. Ligand binding at the cell surface induces dimerization and autophosphorylation of TYRO3 on its intracellular domain that provides docking sites for downstream signaling molecules. Following activation by ligand, interacts with PIK3R1 and thereby enhances PI3-kinase activity. Activates the AKT survival pathway, including nuclear translocation of NF-kappa-B and up-regulation of transcription of NF-kappa-B-regulated genes. TYRO3 signaling plays a role in various processes such as neuron protection from excitotoxic injury, platelet aggregation and cytoskeleton reorganization. Plays also an important role in inhibition of Toll-like receptors (TLRs)-mediated innate immune response by activating STAT1, which selectively induces production of suppressors of cytokine signaling SOCS1 and SOCS3.<ref>PMID:15650770</ref> <ref>PMID:20363878</ref> <ref>PMID:21084607</ref> <ref>PMID:21291561</ref>
-	~~<div style="background-color:#fffaf0;">~~	+
-	~~== Publication Abstract from PubMed ==~~	+
-	We report the discovery of a novel series of spiroindoline-based inhibitors of Sky kinase that bind in the ATP-binding site and exhibit high levels of kinome selectivity through filling the Ala571-subpocket. These inhibitors exhibit moderate oral bioavailability in the rat due to low absorption across the gut wall.	+
-		+
-	Novel and selective spiroindoline-based inhibitors of sky kinase.,Powell NA, Kohrt JT, Filipski KJ, Kaufman M, Sheehan D, Edmunds JE, Delaney A, Wang Y, Bourbonais F, Lee DY, Schwende F, Sun F, McConnell P, Catana C, Chen H, Ohren J, Perrin LA Bioorg Med Chem Lett. 2011 Nov 16. PMID:22119469<ref>PMID:22119469</ref>	+
-		+
-	~~From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>~~	+
-	~~</div>~~	+
-	~~<div class="pdbe-citations 3qup" style="background-color:#fffaf0;"></div~~>	+
	== References ==		== References ==
	<references/>		<references/>
Line 25:		Line 15:
	</StructureSection>		</StructureSection>
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: ~~Lk3 transgenic mice]]~~	+	[[Category: Mus musculus]]
-	~~[[Category: Receptor protein-tyrosine kinase~~]]	+	[[Category: Ohren JF]]
-	[[Category: Ohren~~, J F]]~~	+
-	~~[[Category: Cytoplasmic surface]]~~	+
-	~~[[Category: Gas6 ligand]]~~	+
-	~~[[Category: Kinase domain]]~~	+
-	~~[[Category: Phosphotransfer]]~~	+
-	~~[[Category: Protein kinase inhibitor]]~~	+
-	~~[[Category: Receptor tyrosine kinase]]~~	+
-	~~[[Category: Spirocycle]]~~	+
-	~~[[Category: Transferase-transferase inhibitor complex~~]]	+

OCA at 05:37, 15 June 2022

2022-06-15T05:37:05Z

←Older revision		Revision as of 05:37, 15 June 2022
Line 1:		Line 1:

	==Inhibitor bound structure of the kinase domain of the murine receptor tyrosine kinase TYRO3 (Sky)==		==Inhibitor bound structure of the kinase domain of the murine receptor tyrosine kinase TYRO3 (Sky)==
-	<StructureSection load='3qup' size='340' side='right' caption='[[3qup]], [[Resolution\|resolution]] 1.90Å' scene=''>	+	<StructureSection load='3qup' size='340' side='right'caption='[[3qup]], [[Resolution\|resolution]] 1.90Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[3qup]] is a 1 chain structure with sequence from [~~http~~://en.wikipedia.org/wiki/Lk3_transgenic_mice Lk3 transgenic mice]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3QUP OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=3QUP FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[3qup]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Lk3_transgenic_mice Lk3 transgenic mice]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3QUP OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3QUP FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=LUN:(5-FLUORO-1H-INDOL-2-YL)[(3R)-1-[(3R)-PIPERIDIN-3-YL]SPIRO[INDOLE-3,3-PYRROLIDIN]-1(2H)-YL]METHANONE'>LUN</scene></td></tr>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=LUN:(5-FLUORO-1H-INDOL-2-YL)[(3R)-1-[(3R)-PIPERIDIN-3-YL]SPIRO[INDOLE-3,3-PYRROLIDIN]-1(2H)-YL]METHANONE'>LUN</scene></td></tr>
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">Tyro3, Dtk, Rse ([~~http~~://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10090 LK3 transgenic mice])</td></tr>	+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">Tyro3, Dtk, Rse ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10090 LK3 transgenic mice])</td></tr>
-	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[~~http~~://en.wikipedia.org/wiki/Receptor_protein-tyrosine_kinase Receptor protein-tyrosine kinase], with EC number [~~http~~://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.1 2.7.10.1] </span></td></tr>	+	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[https://en.wikipedia.org/wiki/Receptor_protein-tyrosine_kinase Receptor protein-tyrosine kinase], with EC number [https://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.1 2.7.10.1] </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=3qup FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3qup OCA], [~~http~~://pdbe.org/3qup PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=3qup RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/3qup PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=3qup 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=3qup FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3qup OCA], [https://pdbe.org/3qup PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3qup RCSB], [https://www.ebi.ac.uk/pdbsum/3qup PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3qup ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[[~~http~~://www.uniprot.org/uniprot/TYRO3_MOUSE TYRO3_MOUSE]] Receptor tyrosine kinase that transduces signals from the extracellular matrix into the cytoplasm by binding to several ligands including TULP1 or GAS6. Regulates many physiological processes including cell survival, migration and differentiation. Ligand binding at the cell surface induces dimerization and autophosphorylation of TYRO3 on its intracellular domain that provides docking sites for downstream signaling molecules. Following activation by ligand, interacts with PIK3R1 and thereby enhances PI3-kinase activity. Activates the AKT survival pathway, including nuclear translocation of NF-kappa-B and up-regulation of transcription of NF-kappa-B-regulated genes. TYRO3 signaling plays a role in various processes such as neuron protection from excitotoxic injury, platelet aggregation and cytoskeleton reorganization. Plays also an important role in inhibition of Toll-like receptors (TLRs)-mediated innate immune response by activating STAT1, which selectively induces production of suppressors of cytokine signaling SOCS1 and SOCS3.<ref>PMID:15650770</ref> <ref>PMID:20363878</ref> <ref>PMID:21084607</ref> <ref>PMID:21291561</ref>	+	[[https://www.uniprot.org/uniprot/TYRO3_MOUSE TYRO3_MOUSE]] Receptor tyrosine kinase that transduces signals from the extracellular matrix into the cytoplasm by binding to several ligands including TULP1 or GAS6. Regulates many physiological processes including cell survival, migration and differentiation. Ligand binding at the cell surface induces dimerization and autophosphorylation of TYRO3 on its intracellular domain that provides docking sites for downstream signaling molecules. Following activation by ligand, interacts with PIK3R1 and thereby enhances PI3-kinase activity. Activates the AKT survival pathway, including nuclear translocation of NF-kappa-B and up-regulation of transcription of NF-kappa-B-regulated genes. TYRO3 signaling plays a role in various processes such as neuron protection from excitotoxic injury, platelet aggregation and cytoskeleton reorganization. Plays also an important role in inhibition of Toll-like receptors (TLRs)-mediated innate immune response by activating STAT1, which selectively induces production of suppressors of cytokine signaling SOCS1 and SOCS3.<ref>PMID:15650770</ref> <ref>PMID:20363878</ref> <ref>PMID:21084607</ref> <ref>PMID:21291561</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 24:		Line 24:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Large Structures]]
	[[Category: Lk3 transgenic mice]]		[[Category: Lk3 transgenic mice]]
	[[Category: Receptor protein-tyrosine kinase]]		[[Category: Receptor protein-tyrosine kinase]]

OCA at 22:04, 4 August 2016

2016-08-04T22:04:35Z

←Older revision		Revision as of 22:04, 4 August 2016
Line 1:		Line 1:
		+
	==Inhibitor bound structure of the kinase domain of the murine receptor tyrosine kinase TYRO3 (Sky)==		==Inhibitor bound structure of the kinase domain of the murine receptor tyrosine kinase TYRO3 (Sky)==
	<StructureSection load='3qup' size='340' side='right' caption='[[3qup]], [[Resolution\|resolution]] 1.90Å' scene=''>		<StructureSection load='3qup' size='340' side='right' caption='[[3qup]], [[Resolution\|resolution]] 1.90Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[3qup]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/~~Mus_musculus Mus musculus~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3QUP OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3QUP FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[3qup]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Lk3_transgenic_mice Lk3 transgenic mice]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3QUP OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3QUP FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=LUN:(5-FLUORO-1H-INDOL-2-YL)[(3R)-1-[(3R)-PIPERIDIN-3-YL]SPIRO[INDOLE-3,3-PYRROLIDIN]-1(2H)-YL]METHANONE'>LUN</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=LUN:(5-FLUORO-1H-INDOL-2-YL)[(3R)-1-[(3R)-PIPERIDIN-3-YL]SPIRO[INDOLE-3,3-PYRROLIDIN]-1(2H)-YL]METHANONE'>LUN</scene></td></tr>
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">Tyro3, Dtk, Rse ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10090 ~~Mus musculus~~])</td></tr>	+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">Tyro3, Dtk, Rse ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10090 LK3 transgenic mice])</td></tr>
	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Receptor_protein-tyrosine_kinase Receptor protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.1 2.7.10.1] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Receptor_protein-tyrosine_kinase Receptor protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.1 2.7.10.1] </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=3qup FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3qup OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3qup RCSB], [http://www.ebi.ac.uk/pdbsum/3qup 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=3qup FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3qup OCA], [http://pdbe.org/3qup PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=3qup RCSB], [http://www.ebi.ac.uk/pdbsum/3qup PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=3qup ProSAT]</span></td></tr>
	</table>		</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/TYRO3_MOUSE TYRO3_MOUSE]] Receptor tyrosine kinase that transduces signals from the extracellular matrix into the cytoplasm by binding to several ligands including TULP1 or GAS6. Regulates many physiological processes including cell survival, migration and differentiation. Ligand binding at the cell surface induces dimerization and autophosphorylation of TYRO3 on its intracellular domain that provides docking sites for downstream signaling molecules. Following activation by ligand, interacts with PIK3R1 and thereby enhances PI3-kinase activity. Activates the AKT survival pathway, including nuclear translocation of NF-kappa-B and up-regulation of transcription of NF-kappa-B-regulated genes. TYRO3 signaling plays a role in various processes such as neuron protection from excitotoxic injury, platelet aggregation and cytoskeleton reorganization. Plays also an important role in inhibition of Toll-like receptors (TLRs)-mediated innate immune response by activating STAT1, which selectively induces production of suppressors of cytokine signaling SOCS1 and SOCS3.<ref>PMID:15650770</ref> <ref>PMID:20363878</ref> <ref>PMID:21084607</ref> <ref>PMID:21291561</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 16:		Line 19:
	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 3qup" style="background-color:#fffaf0;"></div>
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Mus musculus~~]]	+	[[Category: Lk3 transgenic mice]]
	[[Category: Receptor protein-tyrosine kinase]]		[[Category: Receptor protein-tyrosine kinase]]
	[[Category: Ohren, J F]]		[[Category: Ohren, J F]]

OCA at 21:51, 3 January 2015

2015-01-03T21:51:48Z

←Older revision		Revision as of 21:51, 3 January 2015
Line 3:		Line 3:
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[3qup]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3QUP OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3QUP FirstGlance]. <br>		<table><tr><td colspan='2'>[[3qup]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3QUP OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3QUP FirstGlance]. <br>
-	</td></tr><tr><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=LUN:(5-FLUORO-1H-INDOL-2-YL)[(3R)-1-[(3R)-PIPERIDIN-3-YL]SPIRO[INDOLE-3,3-PYRROLIDIN]-1(2H)-YL]METHANONE'>LUN</scene><br>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=LUN:(5-FLUORO-1H-INDOL-2-YL)[(3R)-1-[(3R)-PIPERIDIN-3-YL]SPIRO[INDOLE-3,3-PYRROLIDIN]-1(2H)-YL]METHANONE'>LUN</scene></td></tr>
-	<tr><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">Tyro3, Dtk, Rse ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10090 Mus musculus])</td></tr>	+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">Tyro3, Dtk, Rse ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10090 Mus musculus])</td></tr>
-	<tr><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Receptor_protein-tyrosine_kinase Receptor protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.1 2.7.10.1] </span></td></tr>	+	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Receptor_protein-tyrosine_kinase Receptor protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.1 2.7.10.1] </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=3qup FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3qup OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3qup RCSB], [http://www.ebi.ac.uk/pdbsum/3qup 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=3qup FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3qup OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3qup RCSB], [http://www.ebi.ac.uk/pdbsum/3qup PDBsum]</span></td></tr>
-	<table>	+	</table>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 14:		Line 14:
	Novel and selective spiroindoline-based inhibitors of sky kinase.,Powell NA, Kohrt JT, Filipski KJ, Kaufman M, Sheehan D, Edmunds JE, Delaney A, Wang Y, Bourbonais F, Lee DY, Schwende F, Sun F, McConnell P, Catana C, Chen H, Ohren J, Perrin LA Bioorg Med Chem Lett. 2011 Nov 16. PMID:22119469<ref>PMID:22119469</ref>		Novel and selective spiroindoline-based inhibitors of sky kinase.,Powell NA, Kohrt JT, Filipski KJ, Kaufman M, Sheehan D, Edmunds JE, Delaney A, Wang Y, Bourbonais F, Lee DY, Schwende F, Sun F, McConnell P, Catana C, Chen H, Ohren J, Perrin LA Bioorg Med Chem Lett. 2011 Nov 16. PMID:22119469<ref>PMID:22119469</ref>

-	From ~~MEDLINEÂ®~~/~~PubMedÂ®~~, 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>
	== References ==		== References ==
Line 22:		Line 22:
	[[Category: Mus musculus]]		[[Category: Mus musculus]]
	[[Category: Receptor protein-tyrosine kinase]]		[[Category: Receptor protein-tyrosine kinase]]
-	[[Category: Ohren, J F.]]	+	[[Category: Ohren, J F]]
	[[Category: Cytoplasmic surface]]		[[Category: Cytoplasmic surface]]
	[[Category: Gas6 ligand]]		[[Category: Gas6 ligand]]

OCA at 04:44, 5 June 2014

2014-06-05T04:44:17Z

←Older revision		Revision as of 04:44, 5 June 2014
Line 1:		Line 1:
-	[[~~Image:~~3qup.~~png~~\|~~left~~\|~~200px~~]]	+	==Inhibitor bound structure of the kinase domain of the murine receptor tyrosine kinase TYRO3 (Sky)==
		+	<StructureSection load='3qup' size='340' side='right' caption='[[3qup]], [[Resolution\|resolution]] 1.90Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[3qup]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3QUP OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3QUP FirstGlance]. <br>
		+	</td></tr><tr><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=LUN:(5-FLUORO-1H-INDOL-2-YL)[(3R)-1-[(3R)-PIPERIDIN-3-YL]SPIRO[INDOLE-3,3-PYRROLIDIN]-1(2H)-YL]METHANONE'>LUN</scene><br>
		+	<tr><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">Tyro3, Dtk, Rse ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10090 Mus musculus])</td></tr>
		+	<tr><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Receptor_protein-tyrosine_kinase Receptor protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.1 2.7.10.1] </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=3qup FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3qup OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3qup RCSB], [http://www.ebi.ac.uk/pdbsum/3qup PDBsum]</span></td></tr>
		+	<table>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	We report the discovery of a novel series of spiroindoline-based inhibitors of Sky kinase that bind in the ATP-binding site and exhibit high levels of kinome selectivity through filling the Ala571-subpocket. These inhibitors exhibit moderate oral bioavailability in the rat due to low absorption across the gut wall.

-	<!--	+	Novel and selective spiroindoline-based inhibitors of sky kinase.,Powell NA, Kohrt JT, Filipski KJ, Kaufman M, Sheehan D, Edmunds JE, Delaney A, Wang Y, Bourbonais F, Lee DY, Schwende F, Sun F, McConnell P, Catana C, Chen H, Ohren J, Perrin LA Bioorg Med Chem Lett. 2011 Nov 16. PMID:22119469<ref>PMID:22119469</ref>
-	~~The line below this paragraph~~, ~~containing "STRUCTURE_3qup"~~, ~~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_3qup\| PDB=3qup \| SCENE= }}~~	+

-	~~===Inhibitor bound structure~~ of the ~~kinase domain of the murine receptor tyrosine kinase TYRO3 (Sky)===~~	+	From MEDLINEÂ®/PubMedÂ®, a database of the U.S. National Library of Medicine.<br>
-		+	</div>
-		+	== References ==
-	~~<!--~~	+	<references/>
-	~~The line below this paragraph, {{ABSTRACT_PUBMED_22119469}}, adds the Publication Abstract to the page~~	+	__TOC__
-	~~(as it appears on PubMed at http://www~~.~~pubmed~~.~~gov), where 22119469 is the PubMed ID number~~.	+	</StructureSection>
-	-->	+
-	~~{{ABSTRACT_PUBMED_22119469}}~~	+
-		+
-	~~==About this Structure==~~	+
-	~~[[3qup]] is a 1 chain structure with sequence from [http:~~/~~/en.wikipedia.org/wiki/Mus_musculus Mus musculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3QUP OCA].~~	+
-		+
-	==~~Reference~~==	+
-	<~~ref group="xtra">PMID:022119469<~~/~~ref~~><~~references group="xtra"~~/>	+
	[[Category: Mus musculus]]		[[Category: Mus musculus]]
	[[Category: Receptor protein-tyrosine kinase]]		[[Category: Receptor protein-tyrosine kinase]]

OCA at 05:40, 11 January 2012

2012-01-11T05:40:28Z

←Older revision		Revision as of 05:40, 11 January 2012
Line 1:		Line 1:
-	~~'''Unreleased structure'''~~	+	[[Image:3qup.png\|left\|200px]]

-	The ~~entry 3qup~~ is ~~ON HOLD~~ ~~until Paper Publication~~	+	<!--
		+	The line below this paragraph, containing "STRUCTURE_3qup", 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_3qup\| PDB=3qup \| SCENE= }}

-	~~Authors: Ohren, J.F.~~	+	===Inhibitor bound structure of the kinase domain of the murine receptor tyrosine kinase TYRO3 (Sky)===

-	~~Description~~: ~~Inhibitor bound structure of~~ the kinase domain ~~of the murine receptor~~ tyrosine kinase ~~TYRO3 (Sky)~~	+
		+	<!--
		+	The line below this paragraph, {{ABSTRACT_PUBMED_22119469}}, adds the Publication Abstract to the page
		+	(as it appears on PubMed at http://www.pubmed.gov), where 22119469 is the PubMed ID number.
		+	-->
		+	{{ABSTRACT_PUBMED_22119469}}
		+
		+	==About this Structure==
		+	[[3qup]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3QUP OCA].
		+
		+	==Reference==
		+	<ref group="xtra">PMID:022119469</ref><references group="xtra"/>
		+	[[Category: Mus musculus]]
		+	[[Category: Receptor protein-tyrosine kinase]]
		+	[[Category: Ohren, J F.]]
		+	[[Category: Cytoplasmic surface]]
		+	[[Category: Gas6 ligand]]
		+	[[Category: Kinase domain]]
		+	[[Category: Phosphotransfer]]
		+	[[Category: Protein kinase inhibitor]]
		+	[[Category: Receptor tyrosine kinase]]
		+	[[Category: Spirocycle]]
		+	[[Category: Transferase-transferase inhibitor complex]]

OCA at 05:37, 29 June 2011

2011-06-29T05:37:06Z

←Older revision		Revision as of 05:37, 29 June 2011
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 3qup is ON HOLD	+	The entry 3qup is ON HOLD until Paper Publication

	Authors: Ohren, J.F.		Authors: Ohren, J.F.

	Description: Inhibitor bound structure of the kinase domain of the murine receptor tyrosine kinase TYRO3 (Sky)		Description: Inhibitor bound structure of the kinase domain of the murine receptor tyrosine kinase TYRO3 (Sky)

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

2011-03-02T06:45:35Z

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

←Older revision

Revision as of 06:45, 2 March 2011

OCA: New page: '''Unreleased structure''' The entry 3qup is ON HOLD Authors: Ohren, J.F. Description: Inhibitor bound structure of the kinase domain of the murine receptor tyrosine kinase TYRO3 (Sky)

2011-03-02T06:45:34Z

New page: '''Unreleased structure''' The entry 3qup is ON HOLD Authors: Ohren, J.F. Description: Inhibitor bound structure of the kinase domain of the murine receptor tyrosine kinase TYRO3 (Sky)

New page

'''Unreleased structure'''

The entry 3qup is ON HOLD

Authors: Ohren, J.F.

Description: Inhibitor bound structure of the kinase domain of the murine receptor tyrosine kinase TYRO3 (Sky)