4yth - Revision history

OCA at 08:38, 23 October 2024

2024-10-23T08:38:55Z

← Older revision		Revision as of 08:38, 23 October 2024
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	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[4yth]] 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=4YTH OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4YTH FirstGlance]. <br>		<table><tr><td colspan='2'>[[4yth]] 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=4YTH OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4YTH FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=467:N~2~-[2-(5-CHLORO-1H-PYRROLO[2,3-B]PYRIDIN-3-YL)-5-FLUOROPYRIMIDIN-4-YL]-2-METHYL-N-(2,2,2-TRIFLUOROETHYL)-D-ALANINAMIDE'>467</scene>, <scene name='pdbligand=PTR:O-PHOSPHOTYROSINE'>PTR</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]] 2.04Å</td></tr>
			<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=467:N~2~-[2-(5-CHLORO-1H-PYRROLO[2,3-B]PYRIDIN-3-YL)-5-FLUOROPYRIMIDIN-4-YL]-2-METHYL-N-(2,2,2-TRIFLUOROETHYL)-D-ALANINAMIDE'>467</scene>, <scene name='pdbligand=PTR:O-PHOSPHOTYROSINE'>PTR</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=4yth FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4yth OCA], [https://pdbe.org/4yth PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4yth RCSB], [https://www.ebi.ac.uk/pdbsum/4yth PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4yth 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=4yth FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4yth OCA], [https://pdbe.org/4yth PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4yth RCSB], [https://www.ebi.ac.uk/pdbsum/4yth PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4yth ProSAT]</span></td></tr>
	</table>		</table>

OCA at 07:24, 10 May 2023

2023-05-10T07:24:56Z

← Older revision		Revision as of 07:24, 10 May 2023
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	==Discovery of VX-509 (Decernotinib): A Potent and Selective Janus kinase (JAK) 3 Inhibitor for the Treatment of Autoimmune Diseases==		==Discovery of VX-509 (Decernotinib): A Potent and Selective Janus kinase (JAK) 3 Inhibitor for the Treatment of Autoimmune Diseases==
	<StructureSection load='4yth' size='340' side='right' caption='[[4yth]], [[Resolution\|resolution]] 2.04Å' scene=''>		<StructureSection load='4yth' size='340' side='right'caption='[[4yth]], [[Resolution\|resolution]] 2.04Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[4yth]] 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=4YTH OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=4YTH FirstGlance]. <br>		<table><tr><td colspan='2'>[[4yth]] 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=4YTH OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4YTH FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=467:N~2~-[2-(5-CHLORO-1H-PYRROLO[2,3-B]PYRIDIN-3-YL)-5-FLUOROPYRIMIDIN-4-YL]-2-METHYL-N-(2,2,2-TRIFLUOROETHYL)-D-ALANINAMIDE'>467</scene>~~</td></tr>~~		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=467:N~2~-[2-(5-CHLORO-1H-PYRROLO[2,3-B]PYRIDIN-3-YL)-5-FLUOROPYRIMIDIN-4-YL]-2-METHYL-N-(2,2,2-TRIFLUOROETHYL)-D-ALANINAMIDE'>467</scene>, <scene name='pdbligand=PTR:O-PHOSPHOTYROSINE'>PTR</scene></td></tr>
	~~<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat">~~<scene name='pdbligand=PTR:O-PHOSPHOTYROSINE'>PTR</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=4yth FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4yth OCA], [https://pdbe.org/4yth PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4yth RCSB], [https://www.ebi.ac.uk/pdbsum/4yth PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4yth ProSAT]</span></td></tr>
	~~<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4ytc\|4ytc]], [[4ytf\|4ytf]], [[4yti\|4yti]]</td></tr>~~
	~~<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">JAK2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>~~
	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_protein-tyrosine_kinase Non-specific protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.2 2.7.10.2] </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=4yth FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4yth OCA], [~~http~~://pdbe.org/4yth PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=4yth RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/4yth PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=4yth ProSAT]</span></td></tr>
	</table>		</table>
	== Disease ==		== Disease ==
	[~~[http~~://www.uniprot.org/uniprot/JAK2_HUMAN JAK2_HUMAN]] Note=Chromosomal aberrations involving JAK2 are found in both chronic and acute forms of eosinophilic, lymphoblastic and myeloid leukemia. Translocation t(8;9)(p22;p24) with PCM1 links the protein kinase domain of JAK2 to the major portion of PCM1. Translocation t(9;12)(p24;p13) with ETV6. Defects in JAK2 are a cause of susceptibility to Budd-Chiari syndrome (BDCHS) [MIM:[~~http~~://omim.org/entry/600880 600880]]. A syndrome caused by obstruction of hepatic venous outflow involving either the hepatic veins or the terminal segment of the inferior vena cava. Obstructions are generally caused by thrombosis and lead to hepatic congestion and ischemic necrosis. Clinical manifestations observed in the majority of patients include hepatomegaly, right upper quadrant pain and abdominal ascites. Budd-Chiari syndrome is associated with a combination of disease states including primary myeloproliferative syndromes and thrombophilia due to factor V Leiden, protein C deficiency and antithrombin III deficiency. Budd-Chiari syndrome is a rare but typical complication in patients with polycythemia vera. Defects in JAK2 are a cause of polycythemia vera (PV) [MIM:[~~http~~://omim.org/entry/263300 263300]]. A myeloproliferative disorder characterized by abnormal proliferation of all hematopoietic bone marrow elements, erythroid hyperplasia, an absolute increase in total blood volume, but also by myeloid leukocytosis, thrombocytosis and splenomegaly.<ref>PMID:15781101</ref> <ref>PMID:15793561</ref> <ref>PMID:15858187</ref> <ref>PMID:16603627</ref> Defects in JAK2 gene may be the cause of thrombocythemia type 3 (THCYT3) [MIM:[~~http~~://omim.org/entry/614521 614521]]. A myeloproliferative disorder characterized by elevated platelet levels due to sustained proliferation of megakaryocytes, and frequently lead to thrombotic and haemorrhagic complications.<ref>PMID:16325696</ref> <ref>PMID:22397670</ref> Defects in JAK2 are a cause of myelofibrosis (MYELOF) [MIM:[~~http~~://omim.org/entry/254450 254450]]. Myelofibrosis is a disorder characterized by replacement of the bone marrow by fibrous tissue, occurring in association with a myeloproliferative disorder. Clinical manifestations may include anemia, pallor, splenomegaly, hypermetabolic state, petechiae, ecchymosis, bleeding, lymphadenopathy, hepatomegaly, portal hypertension. Defects in JAK2 are a cause of acute myelogenous leukemia (AML) [MIM:[~~http~~://omim.org/entry/601626 601626]]. AML is a malignant disease in which hematopoietic precursors are arrested in an early stage of development.<ref>PMID:16247455</ref>		[https://www.uniprot.org/uniprot/JAK2_HUMAN JAK2_HUMAN] Note=Chromosomal aberrations involving JAK2 are found in both chronic and acute forms of eosinophilic, lymphoblastic and myeloid leukemia. Translocation t(8;9)(p22;p24) with PCM1 links the protein kinase domain of JAK2 to the major portion of PCM1. Translocation t(9;12)(p24;p13) with ETV6. Defects in JAK2 are a cause of susceptibility to Budd-Chiari syndrome (BDCHS) [MIM:[https://omim.org/entry/600880 600880]. A syndrome caused by obstruction of hepatic venous outflow involving either the hepatic veins or the terminal segment of the inferior vena cava. Obstructions are generally caused by thrombosis and lead to hepatic congestion and ischemic necrosis. Clinical manifestations observed in the majority of patients include hepatomegaly, right upper quadrant pain and abdominal ascites. Budd-Chiari syndrome is associated with a combination of disease states including primary myeloproliferative syndromes and thrombophilia due to factor V Leiden, protein C deficiency and antithrombin III deficiency. Budd-Chiari syndrome is a rare but typical complication in patients with polycythemia vera. Defects in JAK2 are a cause of polycythemia vera (PV) [MIM:[https://omim.org/entry/263300 263300]. A myeloproliferative disorder characterized by abnormal proliferation of all hematopoietic bone marrow elements, erythroid hyperplasia, an absolute increase in total blood volume, but also by myeloid leukocytosis, thrombocytosis and splenomegaly.<ref>PMID:15781101</ref> <ref>PMID:15793561</ref> <ref>PMID:15858187</ref> <ref>PMID:16603627</ref> Defects in JAK2 gene may be the cause of thrombocythemia type 3 (THCYT3) [MIM:[https://omim.org/entry/614521 614521]. A myeloproliferative disorder characterized by elevated platelet levels due to sustained proliferation of megakaryocytes, and frequently lead to thrombotic and haemorrhagic complications.<ref>PMID:16325696</ref> <ref>PMID:22397670</ref> Defects in JAK2 are a cause of myelofibrosis (MYELOF) [MIM:[https://omim.org/entry/254450 254450]. Myelofibrosis is a disorder characterized by replacement of the bone marrow by fibrous tissue, occurring in association with a myeloproliferative disorder. Clinical manifestations may include anemia, pallor, splenomegaly, hypermetabolic state, petechiae, ecchymosis, bleeding, lymphadenopathy, hepatomegaly, portal hypertension. Defects in JAK2 are a cause of acute myelogenous leukemia (AML) [MIM:[https://omim.org/entry/601626 601626]. AML is a malignant disease in which hematopoietic precursors are arrested in an early stage of development.<ref>PMID:16247455</ref>
	== Function ==		== Function ==
	[~~[http~~://www.uniprot.org/uniprot/JAK2_HUMAN JAK2_HUMAN]] Non-receptor tyrosine kinase involved in various processes such as cell growth, development, differentiation or histone modifications. Mediates essential signaling events in both innate and adaptive immunity. In the cytoplasm, plays a pivotal role in signal transduction via its association with type I receptors such as growth hormone (GHR), prolactin (PRLR), leptin (LEPR), erythropoietin (EPOR), thrombopoietin (THPO); or type II receptors including IFN-alpha, IFN-beta, IFN-gamma and multiple interleukins. Following ligand-binding to cell surface receptors, phosphorylates specific tyrosine residues on the cytoplasmic tails of the receptor, creating docking sites for STATs proteins. Subsequently, phosphorylates the STATs proteins once they are recruited to the receptor. Phosphorylated STATs then form homodimer or heterodimers and translocate to the nucleus to activate gene transcription. For example, cell stimulation with erythropoietin (EPO) during erythropoiesis leads to JAK2 autophosphorylation, activation, and its association with erythropoietin receptor (EPOR) that becomes phosphorylated in its cytoplasmic domain. Then, STAT5 (STAT5A or STAT5B) is recruited, phosphorylated and activated by JAK2. Once activated, dimerized STAT5 translocates into the nucleus and promotes the transcription of several essential genes involved in the modulation of erythropoiesis. In addition, JAK2 mediates angiotensin-2-induced ARHGEF1 phosphorylation. Plays a role in cell cycle by phosphorylating CDKN1B. Cooperates with TEC through reciprocal phosphorylation to mediate cytokine-driven activation of FOS transcription. In the nucleus, plays a key role in chromatin by specifically mediating phosphorylation of 'Tyr-41' of histone H3 (H3Y41ph), a specific tag that promotes exclusion of CBX5 (HP1 alpha) from chromatin.<ref>PMID:12023369</ref> <ref>PMID:19783980</ref> <ref>PMID:20098430</ref> <ref>PMID:21423214</ref>		[https://www.uniprot.org/uniprot/JAK2_HUMAN JAK2_HUMAN] Non-receptor tyrosine kinase involved in various processes such as cell growth, development, differentiation or histone modifications. Mediates essential signaling events in both innate and adaptive immunity. In the cytoplasm, plays a pivotal role in signal transduction via its association with type I receptors such as growth hormone (GHR), prolactin (PRLR), leptin (LEPR), erythropoietin (EPOR), thrombopoietin (THPO); or type II receptors including IFN-alpha, IFN-beta, IFN-gamma and multiple interleukins. Following ligand-binding to cell surface receptors, phosphorylates specific tyrosine residues on the cytoplasmic tails of the receptor, creating docking sites for STATs proteins. Subsequently, phosphorylates the STATs proteins once they are recruited to the receptor. Phosphorylated STATs then form homodimer or heterodimers and translocate to the nucleus to activate gene transcription. For example, cell stimulation with erythropoietin (EPO) during erythropoiesis leads to JAK2 autophosphorylation, activation, and its association with erythropoietin receptor (EPOR) that becomes phosphorylated in its cytoplasmic domain. Then, STAT5 (STAT5A or STAT5B) is recruited, phosphorylated and activated by JAK2. Once activated, dimerized STAT5 translocates into the nucleus and promotes the transcription of several essential genes involved in the modulation of erythropoiesis. In addition, JAK2 mediates angiotensin-2-induced ARHGEF1 phosphorylation. Plays a role in cell cycle by phosphorylating CDKN1B. Cooperates with TEC through reciprocal phosphorylation to mediate cytokine-driven activation of FOS transcription. In the nucleus, plays a key role in chromatin by specifically mediating phosphorylation of 'Tyr-41' of histone H3 (H3Y41ph), a specific tag that promotes exclusion of CBX5 (HP1 alpha) from chromatin.<ref>PMID:12023369</ref> <ref>PMID:19783980</ref> <ref>PMID:20098430</ref> <ref>PMID:21423214</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
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	</div>		</div>
	<div class="pdbe-citations 4yth" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 4yth" style="background-color:#fffaf0;"></div>

			==See Also==
			*[[Janus kinase 3D structures\|Janus kinase 3D structures]]
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
	[[Category: ~~Human~~]]		[[Category: Homo sapiens]]
	[[Category: ~~Non-specific protein-tyrosine kinase~~]]		[[Category: Large Structures]]
	[[Category: Ledeboer~~, M W~~]]		[[Category: Ledeboer MW]]
	[[Category: Zuccola~~, H J]]~~		[[Category: Zuccola HJ]]
	~~[[Category: Autoimmune]]~~
	~~[[Category: Inhibitor]]~~
	~~[[Category: Jak2 kinase]]~~
	~~[[Category: Jak3 kinase]]~~
	~~[[Category: Transferase-transferase inhibitor complex~~]]

OCA at 16:21, 16 November 2017

2017-11-16T16:21:04Z

← Older revision		Revision as of 16:21, 16 November 2017
Line 3:		Line 3:
	<StructureSection load='4yth' size='340' side='right' caption='[[4yth]], [[Resolution\|resolution]] 2.04Å' scene=''>		<StructureSection load='4yth' size='340' side='right' caption='[[4yth]], [[Resolution\|resolution]] 2.04Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[4yth]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4YTH OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4YTH FirstGlance]. <br>		<table><tr><td colspan='2'>[[4yth]] 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=4YTH OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4YTH FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=467:N~2~-[2-(5-CHLORO-1H-PYRROLO[2,3-B]PYRIDIN-3-YL)-5-FLUOROPYRIMIDIN-4-YL]-2-METHYL-N-(2,2,2-TRIFLUOROETHYL)-D-ALANINAMIDE'>467</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=467:N~2~-[2-(5-CHLORO-1H-PYRROLO[2,3-B]PYRIDIN-3-YL)-5-FLUOROPYRIMIDIN-4-YL]-2-METHYL-N-(2,2,2-TRIFLUOROETHYL)-D-ALANINAMIDE'>467</scene></td></tr>
	<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=PTR:O-PHOSPHOTYROSINE'>PTR</scene></td></tr>		<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=PTR:O-PHOSPHOTYROSINE'>PTR</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4ytc\|4ytc]], [[4ytf\|4ytf]], [[4yti\|4yti]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4ytc\|4ytc]], [[4ytf\|4ytf]], [[4yti\|4yti]]</td></tr>
			<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">JAK2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_protein-tyrosine_kinase Non-specific protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.2 2.7.10.2] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_protein-tyrosine_kinase Non-specific protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.2 2.7.10.2] </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=4yth FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4yth OCA], [http://pdbe.org/4yth PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4yth RCSB], [http://www.ebi.ac.uk/pdbsum/4yth PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4yth ProSAT]</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=4yth FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4yth OCA], [http://pdbe.org/4yth PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4yth RCSB], [http://www.ebi.ac.uk/pdbsum/4yth PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4yth ProSAT]</span></td></tr>
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	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
			[[Category: Human]]
	[[Category: Non-specific protein-tyrosine kinase]]		[[Category: Non-specific protein-tyrosine kinase]]
	[[Category: Ledeboer, M W]]		[[Category: Ledeboer, M W]]

OCA at 06:30, 26 July 2016

2016-07-26T06:30:02Z

← Older revision		Revision as of 06:30, 26 July 2016
Line 1:		Line 1:

	==Discovery of VX-509 (Decernotinib): A Potent and Selective Janus kinase (JAK) 3 Inhibitor for the Treatment of Autoimmune Diseases==		==Discovery of VX-509 (Decernotinib): A Potent and Selective Janus kinase (JAK) 3 Inhibitor for the Treatment of Autoimmune Diseases==
	<StructureSection load='4yth' size='340' side='right' caption='[[4yth]], [[Resolution\|resolution]] 2.04Å' scene=''>		<StructureSection load='4yth' size='340' side='right' caption='[[4yth]], [[Resolution\|resolution]] 2.04Å' scene=''>
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	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4ytc\|4ytc]], [[4ytf\|4ytf]], [[4yti\|4yti]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4ytc\|4ytc]], [[4ytf\|4ytf]], [[4yti\|4yti]]</td></tr>
	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_protein-tyrosine_kinase Non-specific protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.2 2.7.10.2] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_protein-tyrosine_kinase Non-specific protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.2 2.7.10.2] </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=4yth FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4yth OCA], [http://pdbe.org/4yth PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4yth RCSB], [http://www.ebi.ac.uk/pdbsum/4yth 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=4yth FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4yth OCA], [http://pdbe.org/4yth PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4yth RCSB], [http://www.ebi.ac.uk/pdbsum/4yth PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4yth ProSAT]</span></td></tr>
	</table>		</table>
	== Disease ==		== Disease ==

OCA at 06:24, 30 September 2015

2015-09-30T06:24:00Z

← Older revision		Revision as of 06:24, 30 September 2015
Line 7:		Line 7:
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4ytc\|4ytc]], [[4ytf\|4ytf]], [[4yti\|4yti]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4ytc\|4ytc]], [[4ytf\|4ytf]], [[4yti\|4yti]]</td></tr>
	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_protein-tyrosine_kinase Non-specific protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.2 2.7.10.2] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_protein-tyrosine_kinase Non-specific protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.2 2.7.10.2] </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=4yth FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4yth OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4yth RCSB], [http://www.ebi.ac.uk/pdbsum/4yth 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=4yth FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4yth OCA], [http://pdbe.org/4yth PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4yth RCSB], [http://www.ebi.ac.uk/pdbsum/4yth PDBsum]</span></td></tr>
	</table>		</table>
	== Disease ==		== Disease ==
Line 21:		Line 21:
	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 4yth" style="background-color:#fffaf0;"></div>
	== References ==		== References ==
	<references/>		<references/>

OCA at 14:39, 12 August 2015

2015-08-12T14:39:17Z

@@ Line 1: / Line 1: @@
-'''Unreleased structure'''
+==Discovery of VX-509 (Decernotinib): A Potent and Selective Janus kinase (JAK) 3 Inhibitor for the Treatment of Autoimmune Diseases==
-The entry 4yth is ON HOLD  until Paper Publication
+Discovery of VX-509 (Decernotinib): A Potent and Selective Janus kinase (JAK) 3 Inhibitor for the Treatment of Autoimmune Diseases.,Farmer L, Ledeboer MW, Hoock T, Arnost MJ, Bethiel RS, Bennani YL, Black JJ, Brummel CL, Chakilam A, Dorsch WA, Fan B, Cochran J, Halas S, Harrington EM, Hogan JK, Howe D, Huang H, Jacobs DH, Laitinen LM, Liao S, Mahajan S, Marone V, Martinez-Botella G, McCarthy P, Messersmith D, Namchuk M, Oh L, Pierce AC, Raybuck SA, Rugg A, Salituro FG, Saxena K, Shannon D, Shlyakter D, Swenson L, Tian SK, Town C, Wang J, Wang T, Wannamaker MW, Winquist RJ, Zuccola HJ J Med Chem. 2015 Jul 31. PMID:26230873<ref>PMID:26230873</ref>
-Authors: Ledeboer, M.W., Zuccola, H.J.
+From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
+</div>
-Description:
+== References ==
-[[Category: Unreleased Structures]]
+<references/>
-[[Category: Ledeboer, M.W]]
+__TOC__
-[[Category: Zuccola, H.J]]
+</StructureSection>

OCA at 11:21, 15 April 2015

2015-04-15T11:21:13Z

← Older revision		Revision as of 11:21, 15 April 2015
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

	The entry 4yth is ON HOLD		The entry 4yth is ON HOLD until Paper Publication

	Authors: Ledeboer, M.W., Zuccola, H.J.		Authors: Ledeboer, M.W., Zuccola, H.J.

OCA at 11:52, 1 April 2015

2015-04-01T11:52:34Z

← Older revision		Revision as of 11:52, 1 April 2015
Line 3:		Line 3:
	The entry 4yth is ON HOLD		The entry 4yth is ON HOLD

	Authors: ~~ledeboer~~, m. w., ~~zuccola~~, h. j.		Authors: Ledeboer, M.W., Zuccola, H.J.

	Description:		Description:
	[[Category: Unreleased Structures]]		[[Category: Unreleased Structures]]
	[[Category: Ledeboer, M. W]]		[[Category: Ledeboer, M.W]]
	[[Category: Zuccola, H. J]]		[[Category: Zuccola, H.J]]

OCA: Protected "4yth" [edit=sysop:move=sysop]

2015-03-26T12:49:17Z

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

← Older revision	Revision as of 12:49, 26 March 2015
(No difference)

OCA: New page: '''Unreleased structure''' The entry 4yth is ON HOLD Authors: ledeboer, m. w., zuccola, h. j. Description: Category: Unreleased Structures Category: Ledeboer, M. W [[Category:...

2015-03-26T12:49:16Z

New page: '''Unreleased structure''' The entry 4yth is ON HOLD Authors: ledeboer, m. w., zuccola, h. j. Description: Category: Unreleased Structures Category: Ledeboer, M. W [[Category:...

New page

'''Unreleased structure'''

The entry 4yth is ON HOLD

Authors: ledeboer, m. w., zuccola, h. j.

Description:
[[Category: Unreleased Structures]]
[[Category: Ledeboer, M. W]]
[[Category: Zuccola, H. J]]