4ff8 - Revision history

OCA at 11:15, 1 March 2024

2024-03-01T11:15:57Z

←Older revision		Revision as of 11:15, 1 March 2024
Line 4:		Line 4:
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[4ff8]] 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=4FF8 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4FF8 FirstGlance]. <br>		<table><tr><td colspan='2'>[[4ff8]] 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=4FF8 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4FF8 FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=14S:4-(CYCLOPENTYLAMINO)-2-[(2-METHOXYBENZYL)AMINO]-N-[3-(2-OXOPYRROLIDIN-1-YL)PROPYL]PYRIMIDINE-5-CARBOXAMIDE'>14S</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]] 2.4Å</td></tr>
		+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=14S:4-(CYCLOPENTYLAMINO)-2-[(2-METHOXYBENZYL)AMINO]-N-[3-(2-OXOPYRROLIDIN-1-YL)PROPYL]PYRIMIDINE-5-CARBOXAMIDE'>14S</scene></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=4ff8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ff8 OCA], [https://pdbe.org/4ff8 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4ff8 RCSB], [https://www.ebi.ac.uk/pdbsum/4ff8 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4ff8 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=4ff8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ff8 OCA], [https://pdbe.org/4ff8 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4ff8 RCSB], [https://www.ebi.ac.uk/pdbsum/4ff8 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4ff8 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 SAR around a series of 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase. 2-Aminophenethyl analogs demonstrate excellent potency but moderate kinase selectivity, while 2-aminobenzyl analogs that fill the Ala571 subpocket exhibit good inhibition activity and excellent kinase selectivity.
-
-	Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.,Powell NA, Hoffman JK, Ciske FL, Kaufman MD, Kohrt JT, Quin J 3rd, Sheehan DJ, Delaney A, Baxi SM, Catana C, McConnell P, Ohren J, Perrin LA, Edmunds JJ Bioorg Med Chem Lett. 2013 Feb 15;23(4):1046-50. doi: 10.1016/j.bmcl.2012.12.013., Epub 2012 Dec 20. PMID:23312472<ref>PMID:23312472</ref>
-
-	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	</div>
-	<div class="pdbe-citations 4ff8" style="background-color:#fffaf0;"></div>
	== References ==		== References ==
	<references/>		<references/>

OCA at 04:53, 7 October 2022

2022-10-07T04:53:26Z

←Older revision		Revision as of 04:53, 7 October 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='4ff8' size='340' side='right' caption='[[4ff8]], [[Resolution\|resolution]] 2.40Å' scene=''>	+	<StructureSection load='4ff8' size='340' side='right'caption='[[4ff8]], [[Resolution\|resolution]] 2.40Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[4ff8]] 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=4FF8 OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=4FF8 FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[4ff8]] 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=4FF8 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4FF8 FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=14S:4-(CYCLOPENTYLAMINO)-2-[(2-METHOXYBENZYL)AMINO]-N-[3-(2-OXOPYRROLIDIN-1-YL)PROPYL]PYRIMIDINE-5-CARBOXAMIDE'>14S</scene~~></td></tr>~~	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=14S:4-(CYCLOPENTYLAMINO)-2-[(2-METHOXYBENZYL)AMINO]-N-[3-(2-OXOPYRROLIDIN-1-YL)PROPYL]PYRIMIDINE-5-CARBOXAMIDE'>14S</scene></td></tr>
-	~~<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[3qup\|3qup]], [[4feq\|4feq]]</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=4ff8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ff8 OCA], [https://pdbe.org/4ff8 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4ff8 RCSB], [https://www.ebi.ac.uk/pdbsum/4ff8 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4ff8 ProSAT]</span></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='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=4ff8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ff8 OCA], [~~http~~://pdbe.org/4ff8 PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=4ff8 RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/4ff8 PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=4ff8 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 25:		Line 22:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Lk3 transgenic mice~~]]	+	[[Category: Large Structures]]
-	[[Category: ~~Receptor protein-tyrosine kinase~~]]	+	[[Category: Mus musculus]]
-	[[Category: Kohrt, J]]	+	[[Category: Kohrt J]]
-	[[Category: Ohren~~, J F~~]]	+	[[Category: Ohren JF]]
-	[[Category: Perrin~~, L A~~]]	+	[[Category: Perrin LA]]
-	[[Category: Powell~~, N A]]~~	+	[[Category: Powell NA]]
-	~~[[Category: Phosphotransferase]]~~	+
-	~~[[Category: Receptor protein tyrosine kinase]]~~	+
-	~~[[Category: Transferase-transferase inhibitor complex~~]]	+

OCA at 21:28, 5 August 2016

2016-08-05T21:28:43Z

←Older revision		Revision as of 21:28, 5 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='4ff8' size='340' side='right' caption='[[4ff8]], [[Resolution\|resolution]] 2.40Å' scene=''>		<StructureSection load='4ff8' size='340' side='right' caption='[[4ff8]], [[Resolution\|resolution]] 2.40Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[4ff8]] 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=4FF8 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4FF8 FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[4ff8]] 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=4FF8 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4FF8 FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=14S:4-(CYCLOPENTYLAMINO)-2-[(2-METHOXYBENZYL)AMINO]-N-[3-(2-OXOPYRROLIDIN-1-YL)PROPYL]PYRIMIDINE-5-CARBOXAMIDE'>14S</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=14S:4-(CYCLOPENTYLAMINO)-2-[(2-METHOXYBENZYL)AMINO]-N-[3-(2-OXOPYRROLIDIN-1-YL)PROPYL]PYRIMIDINE-5-CARBOXAMIDE'>14S</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[3qup\|3qup]], [[4feq\|4feq]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[3qup\|3qup]], [[4feq\|4feq]]</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=4ff8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ff8 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4ff8 RCSB], [http://www.ebi.ac.uk/pdbsum/4ff8 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=4ff8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ff8 OCA], [http://pdbe.org/4ff8 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4ff8 RCSB], [http://www.ebi.ac.uk/pdbsum/4ff8 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4ff8 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 4ff8" 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: Kohrt, J]]		[[Category: Kohrt, J]]

OCA at 22:03, 25 December 2014

2014-12-25T22:03:08Z

←Older revision		Revision as of 22:03, 25 December 2014
Line 9:		Line 9:
	<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=4ff8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ff8 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4ff8 RCSB], [http://www.ebi.ac.uk/pdbsum/4ff8 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=4ff8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ff8 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4ff8 RCSB], [http://www.ebi.ac.uk/pdbsum/4ff8 PDBsum]</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 ==

OCA at 08:31, 18 December 2014

2014-12-18T08:31:41Z

←Older revision		Revision as of 08:31, 18 December 2014
Line 1:		Line 1:
-	~~{{STRUCTURE_4ff8\| PDB=4ff8 \| SCENE= }}~~	+	==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='4ff8' size='340' side='right' caption='[[4ff8]], [[Resolution\|resolution]] 2.40Å' scene=''>
-	~~{{ABSTRACT_PUBMED_23312472}}~~	+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[4ff8]] 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=4FF8 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4FF8 FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=14S:4-(CYCLOPENTYLAMINO)-2-[(2-METHOXYBENZYL)AMINO]-N-[3-(2-OXOPYRROLIDIN-1-YL)PROPYL]PYRIMIDINE-5-CARBOXAMIDE'>14S</scene></td></tr>
		+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[3qup\|3qup]], [[4feq\|4feq]]</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='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=4ff8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ff8 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4ff8 RCSB], [http://www.ebi.ac.uk/pdbsum/4ff8 PDBsum]</span></td></tr>
		+	</table>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	We report the SAR around a series of 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase. 2-Aminophenethyl analogs demonstrate excellent potency but moderate kinase selectivity, while 2-aminobenzyl analogs that fill the Ala571 subpocket exhibit good inhibition activity and excellent kinase selectivity.

-	~~==About this Structure==~~	+	Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.,Powell NA, Hoffman JK, Ciske FL, Kaufman MD, Kohrt JT, Quin J 3rd, Sheehan DJ, Delaney A, Baxi SM, Catana C, McConnell P, Ohren J, Perrin LA, Edmunds JJ Bioorg Med Chem Lett. 2013 Feb 15;23(4):1046-50. doi: 10.1016/j.bmcl.2012.12.013., Epub 2012 Dec 20. PMID:23312472<ref>PMID:23312472</ref>
-	~~[[4ff8]] 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~~=~~4FF8 OCA].~~	+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
	[[Category: Mus musculus]]		[[Category: Mus musculus]]
	[[Category: Receptor protein-tyrosine kinase]]		[[Category: Receptor protein-tyrosine kinase]]
-	[[Category: Kohrt, J.]]	+	[[Category: Kohrt, J]]
-	[[Category: Ohren, J F.]]	+	[[Category: Ohren, J F]]
-	[[Category: Perrin, L A.]]	+	[[Category: Perrin, L A]]
-	[[Category: Powell, N A.]]	+	[[Category: Powell, N A]]
	[[Category: Phosphotransferase]]		[[Category: Phosphotransferase]]
	[[Category: Receptor protein tyrosine kinase]]		[[Category: Receptor protein tyrosine kinase]]
	[[Category: Transferase-transferase inhibitor complex]]		[[Category: Transferase-transferase inhibitor complex]]

OCA at 10:23, 13 March 2013

2013-03-13T10:23:34Z

←Older revision		Revision as of 10:23, 13 March 2013
Line 1:		Line 1:
-	~~'''Unreleased~~ structure~~'''~~	+	{{STRUCTURE_4ff8\| PDB=4ff8 \| SCENE= }}
		+	===Inhibitor bound structure of the kinase domain of the murine receptor tyrosine kinase TYRO3 (Sky)===
		+	{{ABSTRACT_PUBMED_23312472}}

-	~~The entry~~ 4ff8 is ~~ON HOLD~~	+	==About this Structure==
-		+	[[4ff8]] 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=4FF8 OCA].
-	~~Authors~~: ~~Ohren, J~~.F.~~, Powell, N~~.A., Kohrt, J., Perrin, L.A.	+	[[Category: Mus musculus]]
-		+	[[Category: Receptor protein-tyrosine kinase]]
-	~~Description~~: ~~Inhibitor bound structure of the kinase domain of the murine receptor~~ tyrosine kinase ~~TYRO3 (Sky)~~	+	[[Category: Kohrt, J.]]
		+	[[Category: Ohren, J F.]]
		+	[[Category: Perrin, L A.]]
		+	[[Category: Powell, N A.]]
		+	[[Category: Phosphotransferase]]
		+	[[Category: Receptor protein tyrosine kinase]]
		+	[[Category: Transferase-transferase inhibitor complex]]

OCA at 06:27, 17 October 2012

2012-10-17T06:27:59Z

←Older revision		Revision as of 06:27, 17 October 2012
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 4ff8 is ON HOLD ~~until sometime in the future~~	+	The entry 4ff8 is ON HOLD

	Authors: Ohren, J.F., Powell, N.A., Kohrt, J., Perrin, L.A.		Authors: Ohren, J.F., Powell, N.A., Kohrt, J., Perrin, L.A.

	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 at 06:44, 25 July 2012

2012-07-25T06:44:51Z

←Older revision		Revision as of 06:44, 25 July 2012
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 4ff8 is ON HOLD	+	The entry 4ff8 is ON HOLD until sometime in the future

	Authors: Ohren, J.F., Powell, N.A., Kohrt, J., Perrin, L.A.		Authors: Ohren, J.F., Powell, N.A., Kohrt, J., Perrin, L.A.

	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 "4ff8" [edit=sysop:move=sysop]

2012-06-06T07:23:52Z

Protected "4ff8" [edit=sysop:move=sysop]

←Older revision

Revision as of 07:23, 6 June 2012

OCA: New page: '''Unreleased structure''' The entry 4ff8 is ON HOLD Authors: Ohren, J.F., Powell, N.A., Kohrt, J., Perrin, L.A. Description: Inhibitor bound structure of the kinase domain of the muri...

2012-06-06T07:23:51Z

New page: '''Unreleased structure''' The entry 4ff8 is ON HOLD Authors: Ohren, J.F., Powell, N.A., Kohrt, J., Perrin, L.A. Description: Inhibitor bound structure of the kinase domain of the muri...

New page

'''Unreleased structure'''

The entry 4ff8 is ON HOLD

Authors: Ohren, J.F., Powell, N.A., Kohrt, J., Perrin, L.A.

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