2xp2 - Revision history

OCA at 10:36, 20 December 2023

2023-12-20T10:36:13Z

← Older revision		Revision as of 10:36, 20 December 2023
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	<StructureSection load='2xp2' size='340' side='right'caption='[[2xp2]], [[Resolution\|resolution]] 1.90Å' scene=''>		<StructureSection load='2xp2' size='340' side='right'caption='[[2xp2]], [[Resolution\|resolution]] 1.90Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[2xp2]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/~~Human Human~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2XP2 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2XP2 FirstGlance]. <br>		<table><tr><td colspan='2'>[[2xp2]] 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=2XP2 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2XP2 FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=VGH:3-[(1R)-1-(2,6-DICHLORO-3-FLUOROPHENYL)ETHOXY]-5-(1-PIPERIDIN-4-YL-1H-PYRAZOL-4-YL)PYRIDIN-2-AMINE'>VGH</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='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='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=VGH:3-[(1R)-1-(2,6-DICHLORO-3-FLUOROPHENYL)ETHOXY]-5-(1-PIPERIDIN-4-YL-1H-PYRAZOL-4-YL)PYRIDIN-2-AMINE'>VGH</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=2xp2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2xp2 OCA], [https://pdbe.org/2xp2 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2xp2 RCSB], [https://www.ebi.ac.uk/pdbsum/2xp2 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2xp2 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=2xp2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2xp2 OCA], [https://pdbe.org/2xp2 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2xp2 RCSB], [https://www.ebi.ac.uk/pdbsum/2xp2 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2xp2 ProSAT]</span></td></tr>
	</table>		</table>
			== Disease ==
			[https://www.uniprot.org/uniprot/ALK_HUMAN ALK_HUMAN] Note=A chromosomal aberration involving ALK is found in a form of non-Hodgkin lymphoma. Translocation t(2;5)(p23;q35) with NPM1. The resulting chimeric NPM1-ALK protein homodimerize and the kinase becomes constitutively activated. The constitutively active fusion proteins are responsible for 5-10% of non-Hodgkin lymphomas. Note=A chromosomal aberration involving ALK is associated with inflammatory myofibroblastic tumors (IMTs). Translocation t(2;11)(p23;p15) with CARS; translocation t(2;4)(p23;q21) with SEC31A. Note=A chromosomal aberration involving ALK is associated with anaplastic large-cell lymphoma (ALCL). Translocation t(2;17)(p23;q25) with ALO17. Defects in ALK are the cause of susceptibility to neuroblastoma type 3 (NBLST3) [MIM:[https://omim.org/entry/613014 613014]. Neuroblastoma is a common neoplasm of early childhood arising from embryonic cells that form the primitive neural crest and give rise to the adrenal medulla and the sympathetic nervous system.<ref>PMID:18724359</ref> <ref>PMID:18923523</ref> <ref>PMID:18923525</ref> Note=The ALK signaling pathway plays an important role in glioblastoma, the most common malignant brain tumor of adults and one of the most lethal cancers. It regulates both glioblastoma migration and growth.
			== Function ==
			[https://www.uniprot.org/uniprot/ALK_HUMAN ALK_HUMAN] Neuronal orphan receptor tyrosine kinase that is essentially and transiently expressed in specific regions of the central and peripheral nervous systems and plays an important role in the genesis and differentiation of the nervous system. Transduces signals from ligands at the cell surface, through specific activation of the mitogen-activated protein kinase (MAPK) pathway. Phosphorylates almost exclusively at the first tyrosine of the Y-x-x-x-Y-Y motif. Following activation by ligand, ALK induces tyrosine phosphorylation of CBL, FRS2, IRS1 and SHC1, as well as of the MAP kinases MAPK1/ERK2 and MAPK3/ERK1. Acts as a receptor for ligands pleiotrophin (PTN), a secreted growth factor, and midkine (MDK), a PTN-related factor, thus participating in PTN and MDK signal transduction. PTN-binding induces MAPK pathway activation, which is important for the anti-apoptotic signaling of PTN and regulation of cell proliferation. MDK-binding induces phosphorylation of the ALK target insulin receptor substrate (IRS1), activates mitogen-activated protein kinases (MAPKs) and PI3-kinase, resulting also in cell proliferation induction. Drives NF-kappa-B activation, probably through IRS1 and the activation of the AKT serine/threonine kinase. Recruitment of IRS1 to activated ALK and the activation of NF-kappa-B are essential for the autocrine growth and survival signaling of MDK.<ref>PMID:11387242</ref> <ref>PMID:11121404</ref> <ref>PMID:11278720</ref> <ref>PMID:11809760</ref> <ref>PMID:12107166</ref> <ref>PMID:12122009</ref> <ref>PMID:15226403</ref> <ref>PMID:15908427</ref> <ref>PMID:16317043</ref> <ref>PMID:17274988</ref> <ref>PMID:16878150</ref>
	== Evolutionary Conservation ==		== Evolutionary Conservation ==
	[[Image:Consurf_key_small.gif\|200px\|right]]		[[Image:Consurf_key_small.gif\|200px\|right]]
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	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
	[[Category: ~~Human~~]]		[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
	~~[[Category: Receptor protein-tyrosine kinase]]~~		[[Category: Brooun A]]
	[[Category: Brooun, A]]		[[Category: Cui JJ]]
	[[Category: Cui~~, J J~~]]		[[Category: Deng Y]]
	[[Category: Deng, Y]]		[[Category: Liu W]]
	[[Category: Liu, W]]		[[Category: Marrone T]]
	[[Category: Marrone, T]]		[[Category: McTigue M]]
	[[Category: McTigue, M]]		[[Category: Timofeevski S]]
	[[Category: Timofeevski, S]]
	~~[[Category: Crizotinib]]~~
	~~[[Category: Transferase~~]]

OCA at 14:52, 17 November 2021

2021-11-17T14:52:27Z

← Older revision		Revision as of 14:52, 17 November 2021
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	<StructureSection load='2xp2' size='340' side='right'caption='[[2xp2]], [[Resolution\|resolution]] 1.90Å' scene=''>		<StructureSection load='2xp2' size='340' side='right'caption='[[2xp2]], [[Resolution\|resolution]] 1.90Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[2xp2]] 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=2XP2 OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=2XP2 FirstGlance]. <br>		<table><tr><td colspan='2'>[[2xp2]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2XP2 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2XP2 FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=VGH:3-[(1R)-1-(2,6-DICHLORO-3-FLUOROPHENYL)ETHOXY]-5-(1-PIPERIDIN-4-YL-1H-PYRAZOL-4-YL)PYRIDIN-2-AMINE'>VGH</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=VGH:3-[(1R)-1-(2,6-DICHLORO-3-FLUOROPHENYL)ETHOXY]-5-(1-PIPERIDIN-4-YL-1H-PYRAZOL-4-YL)PYRIDIN-2-AMINE'>VGH</scene></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=2xp2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2xp2 OCA], [~~http~~://pdbe.org/2xp2 PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=2xp2 RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/2xp2 PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=2xp2 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=2xp2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2xp2 OCA], [https://pdbe.org/2xp2 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2xp2 RCSB], [https://www.ebi.ac.uk/pdbsum/2xp2 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2xp2 ProSAT]</span></td></tr>
	</table>		</table>
	== Evolutionary Conservation ==		== Evolutionary Conservation ==
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	==See Also==		==See Also==
	*[[Tyrosine kinase\|Tyrosine kinase]]		*[[Tyrosine kinase 3D structures\|Tyrosine kinase 3D structures]]
	== References ==		== References ==
	<references/>		<references/>

OCA at 12:24, 10 May 2019

2019-05-10T12:24:46Z

← Older revision		Revision as of 12:24, 10 May 2019
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	==Structure of the Human Anaplastic Lymphoma Kinase in Complex with Crizotinib (PF-02341066)==		==Structure of the Human Anaplastic Lymphoma Kinase in Complex with Crizotinib (PF-02341066)==
	<StructureSection load='2xp2' size='340' side='right' caption='[[2xp2]], [[Resolution\|resolution]] 1.90Å' scene=''>		<StructureSection load='2xp2' size='340' side='right'caption='[[2xp2]], [[Resolution\|resolution]] 1.90Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[2xp2]] 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=2XP2 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2XP2 FirstGlance]. <br>		<table><tr><td colspan='2'>[[2xp2]] 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=2XP2 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2XP2 FirstGlance]. <br>
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	</StructureSection>		</StructureSection>
	[[Category: Human]]		[[Category: Human]]
			[[Category: Large Structures]]
	[[Category: Receptor protein-tyrosine kinase]]		[[Category: Receptor protein-tyrosine kinase]]
	[[Category: Brooun, A]]		[[Category: Brooun, A]]

OCA at 09:32, 10 October 2018

2018-10-10T09:32:33Z

← Older revision		Revision as of 09:32, 10 October 2018
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	==~~STRUCTURE OF THE HUMAN ANAPLASTIC LYMPHOMA KINASE IN COMPLEX WITH CRIZOTINIB~~ (PF-02341066)==		==Structure of the Human Anaplastic Lymphoma Kinase in Complex with Crizotinib (PF-02341066)==
	<StructureSection load='2xp2' size='340' side='right' caption='[[2xp2]], [[Resolution\|resolution]] 1.90Å' scene=''>		<StructureSection load='2xp2' size='340' side='right' caption='[[2xp2]], [[Resolution\|resolution]] 1.90Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
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	Check<jmol>		Check<jmol>
	<jmolCheckbox>		<jmolCheckbox>
	<scriptWhenChecked>select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/xp/2xp2_consurf.spt"</scriptWhenChecked>		<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/xp/2xp2_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>
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	[[Category: Liu, W]]		[[Category: Liu, W]]
	[[Category: Marrone, T]]		[[Category: Marrone, T]]
	[[Category: ~~Mctigue~~, M]]		[[Category: McTigue, M]]
	[[Category: Timofeevski, S]]		[[Category: Timofeevski, S]]
	[[Category: Crizotinib]]		[[Category: Crizotinib]]
	[[Category: Transferase]]		[[Category: Transferase]]

OCA at 23:40, 4 August 2016

2016-08-04T23:40:08Z

← Older revision		Revision as of 23:40, 4 August 2016
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	==STRUCTURE OF THE HUMAN ANAPLASTIC LYMPHOMA KINASE IN COMPLEX WITH CRIZOTINIB (PF-02341066)==		==STRUCTURE OF THE HUMAN ANAPLASTIC LYMPHOMA KINASE IN COMPLEX WITH CRIZOTINIB (PF-02341066)==
	<StructureSection load='2xp2' size='340' side='right' caption='[[2xp2]], [[Resolution\|resolution]] 1.90Å' scene=''>		<StructureSection load='2xp2' size='340' side='right' caption='[[2xp2]], [[Resolution\|resolution]] 1.90Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[2xp2]] 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=2XP2 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2XP2 FirstGlance]. <br>		<table><tr><td colspan='2'>[[2xp2]] 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=2XP2 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2XP2 FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=VGH:3-[(1R)-1-(2,6-DICHLORO-3-FLUOROPHENYL)ETHOXY]-5-(1-PIPERIDIN-4-YL-1H-PYRAZOL-4-YL)PYRIDIN-2-AMINE'>VGH</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=VGH:3-[(1R)-1-(2,6-DICHLORO-3-FLUOROPHENYL)ETHOXY]-5-(1-PIPERIDIN-4-YL-1H-PYRAZOL-4-YL)PYRIDIN-2-AMINE'>VGH</scene></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=2xp2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2xp2 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2xp2 RCSB], [http://www.ebi.ac.uk/pdbsum/2xp2 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=2xp2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2xp2 OCA], [http://pdbe.org/2xp2 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2xp2 RCSB], [http://www.ebi.ac.uk/pdbsum/2xp2 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=2xp2 ProSAT]</span></td></tr>
	</table>		</table>
	== Evolutionary Conservation ==		== Evolutionary Conservation ==
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	<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=2xp2 ConSurf].
	<div style="clear:both"></div>		<div style="clear:both"></div>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
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	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 2xp2" style="background-color:#fffaf0;"></div>

	==See Also==		==See Also==
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	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
	[[Category: ~~Homo sapiens~~]]		[[Category: Human]]
	[[Category: Receptor protein-tyrosine kinase]]		[[Category: Receptor protein-tyrosine kinase]]
	[[Category: Brooun, A]]		[[Category: Brooun, A]]

OCA at 12:44, 18 December 2014

2014-12-18T12:44:53Z

← Older revision		Revision as of 12:44, 18 December 2014
Line 1:		Line 1:
	~~{{STRUCTURE_2xp2\| PDB=2xp2 \| SCENE= }}~~		==STRUCTURE OF THE HUMAN ANAPLASTIC LYMPHOMA KINASE IN COMPLEX WITH CRIZOTINIB (PF-02341066)==
	===STRUCTURE OF THE HUMAN ANAPLASTIC LYMPHOMA KINASE IN COMPLEX WITH CRIZOTINIB (PF-02341066)===		<StructureSection load='2xp2' size='340' side='right' caption='[[2xp2]], [[Resolution\|resolution]] 1.90Å' scene=''>
	~~{{ABSTRACT_PUBMED_21812414}}~~		== Structural highlights ==
			<table><tr><td colspan='2'>[[2xp2]] 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=2XP2 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2XP2 FirstGlance]. <br>
			</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=VGH:3-[(1R)-1-(2,6-DICHLORO-3-FLUOROPHENYL)ETHOXY]-5-(1-PIPERIDIN-4-YL-1H-PYRAZOL-4-YL)PYRIDIN-2-AMINE'>VGH</scene></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=2xp2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2xp2 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2xp2 RCSB], [http://www.ebi.ac.uk/pdbsum/2xp2 PDBsum]</span></td></tr>
			</table>
			== 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/xp/2xp2_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 ==
			Because of the critical roles of aberrant signaling in cancer, both c-MET and ALK receptor tyrosine kinases are attractive oncology targets for therapeutic intervention. The cocrystal structure of 3 (PHA-665752), bound to c-MET kinase domain, revealed a novel ATP site environment, which served as the target to guide parallel, multiattribute drug design. A novel 2-amino-5-aryl-3-benzyloxypyridine series was created to more effectively make the key interactions achieved with 3. In the novel series, the 2-aminopyridine core allowed a 3-benzyloxy group to reach into the same pocket as the 2,6-dichlorophenyl group of 3 via a more direct vector and thus with a better ligand efficiency (LE). Further optimization of the lead series generated the clinical candidate crizotinib (PF-02341066), which demonstrated potent in vitro and in vivo c-MET kinase and ALK inhibition, effective tumor growth inhibition, and good pharmaceutical properties.

	~~==About this~~ Structure==		Structure Based Drug Design of Crizotinib (PF-02341066), a Potent and Selective Dual Inhibitor of Mesenchymal-Epithelial Transition Factor (c-MET) Kinase and Anaplastic Lymphoma Kinase (ALK).,Cui JJ, Tran-Dube M, Shen H, Nambu M, Kung PP, Pairish M, Jia L, Meng J, Funk L, Botrous I, McTigue M, Grodsky N, Ryan K, Padrique E, Alton G, Timofeevski S, Yamazaki S, Li Q, Zou H, Christensen J, Mroczkowski B, Bender S, Kania RS, Edwards MP J Med Chem. 2011 Sep 22;54(18):6342-6363. Epub 2011 Aug 18. PMID:21812414<ref>PMID:21812414</ref>
	~~[[2xp2]] 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=2XP2 OCA].~~

	==~~Reference~~==		From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
	~~<ref group~~=~~"xtra">PMID:021812414</ref>~~<references ~~group="xtra"~~/><~~references~~/>		</div>

			==See Also==
			*[[Tyrosine kinase\|Tyrosine kinase]]
			== References ==
			<references/>
			__TOC__
			</StructureSection>
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
	[[Category: Receptor protein-tyrosine kinase]]		[[Category: Receptor protein-tyrosine kinase]]
	[[Category: Brooun, A.]]		[[Category: Brooun, A]]
	[[Category: Cui, J J.]]		[[Category: Cui, J J]]
	[[Category: Deng, Y.]]		[[Category: Deng, Y]]
	[[Category: Liu, W.]]		[[Category: Liu, W]]
	[[Category: Marrone, T.]]		[[Category: Marrone, T]]
	[[Category: Mctigue, M.]]		[[Category: Mctigue, M]]
	[[Category: Timofeevski, S.]]		[[Category: Timofeevski, S]]
	[[Category: Crizotinib]]		[[Category: Crizotinib]]
	[[Category: Transferase]]		[[Category: Transferase]]

OCA at 05:04, 25 March 2013

2013-03-25T05:04:20Z

← Older revision		Revision as of 05:04, 25 March 2013
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	~~[[Image:2xp2.png\|left\|200px]]~~

	~~<!--~~
	~~The line below this paragraph, containing "STRUCTURE_2xp2", 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_2xp2\| PDB=2xp2 \| SCENE= }}		{{STRUCTURE_2xp2\| PDB=2xp2 \| SCENE= }}

	===STRUCTURE OF THE HUMAN ANAPLASTIC LYMPHOMA KINASE IN COMPLEX WITH CRIZOTINIB (PF-02341066)===		===STRUCTURE OF THE HUMAN ANAPLASTIC LYMPHOMA KINASE IN COMPLEX WITH CRIZOTINIB (PF-02341066)===


	~~<!--~~
	~~The line below this paragraph, {{ABSTRACT_PUBMED_21812414}}, adds the Publication Abstract to the page~~
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	==Reference==		==Reference==
	<ref group="xtra">PMID:021812414</ref><references group="xtra"/>		<ref group="xtra">PMID:021812414</ref><references group="xtra"/><references/>
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
	[[Category: Receptor protein-tyrosine kinase]]		[[Category: Receptor protein-tyrosine kinase]]

OCA: Protected "2xp2" [edit=sysop:move=sysop]

2011-09-28T04:48:47Z

Protected "2xp2" [edit=sysop:move=sysop]

← Older revision	Revision as of 04:48, 28 September 2011
(No difference)

OCA at 04:48, 28 September 2011

2011-09-28T04:48:45Z

← Older revision		Revision as of 04:48, 28 September 2011
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	~~{{Seed}}~~		[[Image:2xp2.png\|left\|200px]]
	[[Image:2xp2.~~jpg~~\|left\|200px]]

	<!--		<!--
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	===STRUCTURE OF THE HUMAN ANAPLASTIC LYMPHOMA KINASE IN COMPLEX WITH CRIZOTINIB (PF-02341066)===		===STRUCTURE OF THE HUMAN ANAPLASTIC LYMPHOMA KINASE IN COMPLEX WITH CRIZOTINIB (PF-02341066)===


			<!--
			The line below this paragraph, {{ABSTRACT_PUBMED_21812414}}, adds the Publication Abstract to the page
			(as it appears on PubMed at http://www.pubmed.gov), where 21812414 is the PubMed ID number.
			-->
			{{ABSTRACT_PUBMED_21812414}}

	==About this Structure==		==About this Structure==
	~~2XP2~~ 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=2XP2 OCA].		[[2xp2]] 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=2XP2 OCA].

			==Reference==
			<ref group="xtra">PMID:021812414</ref><references group="xtra"/>
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
	[[Category: Receptor protein-tyrosine kinase]]		[[Category: Receptor protein-tyrosine kinase]]
	[[Category: Brooun, A.]]		[[Category: Brooun, A.]]
	[[Category: Cui, J.]]		[[Category: Cui, J J.]]
	[[Category: Deng, Y.]]		[[Category: Deng, Y.]]
	[[Category: Liu, W.]]		[[Category: Liu, W.]]
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	[[Category: Crizotinib]]		[[Category: Crizotinib]]
	[[Category: Transferase]]		[[Category: Transferase]]

	~~''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Sep 15 10:46:50 2010''~~

OCA at 07:38, 15 September 2010

2010-09-15T07:38:10Z

@@ Line 1: / Line 1: @@
-'''Unreleased structure'''
+{{Seed}}
-The entry 2xp2 is ON HOLD
+<!--
-Authors: McTigue, M., Deng, Y., Liu, W., Brooun, A., Timofeevski, S., Marrone, T., Cui, J.
+===STRUCTURE OF THE HUMAN ANAPLASTIC LYMPHOMA KINASE IN COMPLEX WITH CRIZOTINIB (PF-02341066)===
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Sep  1 09:29:12 2010''
+==About this Structure==