2wgj - Revision history

OCA at 15:55, 13 December 2023

OCA — Wed, 13 Dec 2023 15:55:10 GMT

←Older revision		Revision as of 15:55, 13 December 2023
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	<StructureSection load='2wgj' size='340' side='right'caption='[[2wgj]], [[Resolution\|resolution]] 2.00Å' scene=''>		<StructureSection load='2wgj' size='340' side='right'caption='[[2wgj]], [[Resolution\|resolution]] 2.00Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[2wgj]] 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=2WGJ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2WGJ FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[2wgj]] 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=2WGJ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2WGJ 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]] 2Å</td></tr>
-	<tr id='~~related~~'><td class="sblockLbl"><b>[[~~Related_structure~~\|~~Related~~:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[1r1w\|1r1w]], [[1ux3\|1ux3]], [[1fyr\|1fyr]], [[2wd1\|2wd1]], [[2cew\|2cew]], [[1shy\|1shy]], [[2uzx\|2uzx]], [[2uzy\|2uzy]], [[2g15\|2g15]], [[1ssl\|1ssl]], [[1r0p\|1r0p]]</div></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'>[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=2wgj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2wgj OCA], [https://pdbe.org/2wgj PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2wgj RCSB], [https://www.ebi.ac.uk/pdbsum/2wgj PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2wgj 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=2wgj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2wgj OCA], [https://pdbe.org/2wgj PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2wgj RCSB], [https://www.ebi.ac.uk/pdbsum/2wgj PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2wgj ProSAT]</span></td></tr>
	</table>		</table>
		+	== Disease ==
		+	[https://www.uniprot.org/uniprot/MET_HUMAN MET_HUMAN] Note=Activation of MET after rearrangement with the TPR gene produces an oncogenic protein. Note=Defects in MET may be associated with gastric cancer. Defects in MET are a cause of hepatocellular carcinoma (HCC) [MIM:[https://omim.org/entry/114550 114550].<ref>PMID:9927037</ref> Defects in MET are a cause of renal cell carcinoma papillary (RCCP) [MIM:[https://omim.org/entry/605074 605074]. It is a subtype of renal cell carcinoma tending to show a tubulo-papillary architecture formed by numerous, irregular, finger-like projections of connective tissue. Renal cell carcinoma is a heterogeneous group of sporadic or hereditary carcinoma derived from cells of the proximal renal tubular epithelium. It is subclassified into common renal cell carcinoma (clear cell, non-papillary carcinoma), papillary renal cell carcinoma, chromophobe renal cell carcinoma, collecting duct carcinoma with medullary carcinoma of the kidney, and unclassified renal cell carcinoma.<ref>PMID:9140397</ref> <ref>PMID:9563489</ref> <ref>PMID:10433944</ref> <ref>PMID:10417759</ref> <ref>PMID:10327054</ref> Note=A common allele in the promoter region of the MET shows genetic association with susceptibility to autism in some families. Functional assays indicate a decrease in MET promoter activity and altered binding of specific transcription factor complexes. Note=MET activating mutations may be involved in the development of a highly malignant, metastatic syndrome known as cancer of unknown primary origin (CUP) or primary occult malignancy. Systemic neoplastic spread is generally a late event in cancer progression. However, in some instances, distant dissemination arises at a very early stage, so that metastases reach clinical relevance before primary lesions. Sometimes, the primary lesions cannot be identified in spite of the progresses in the diagnosis of malignancies.<ref>PMID:20949619</ref>
		+	== Function ==
		+	[https://www.uniprot.org/uniprot/MET_HUMAN MET_HUMAN] Receptor tyrosine kinase that transduces signals from the extracellular matrix into the cytoplasm by binding to hepatocyte growth factor/HGF ligand. Regulates many physiological processes including proliferation, scattering, morphogenesis and survival. Ligand binding at the cell surface induces autophosphorylation of MET on its intracellular domain that provides docking sites for downstream signaling molecules. Following activation by ligand, interacts with the PI3-kinase subunit PIK3R1, PLCG1, SRC, GRB2, STAT3 or the adapter GAB1. Recruitment of these downstream effectors by MET leads to the activation of several signaling cascades including the RAS-ERK, PI3 kinase-AKT, or PLCgamma-PKC. The RAS-ERK activation is associated with the morphogenetic effects while PI3K/AKT coordinates prosurvival effects. During embryonic development, MET signaling plays a role in gastrulation, development and migration of muscles and neuronal precursors, angiogenesis and kidney formation. In adults, participates in wound healing as well as organ regeneration and tissue remodeling. Promotes also differentiation and proliferation of hematopoietic cells.<ref>PMID:1846706</ref> <ref>PMID:8182137</ref> <ref>PMID:15314156</ref> Acts as a receptor for Listeria internalin inlB, mediating entry of the pathogen into cells.<ref>PMID:1846706</ref> <ref>PMID:8182137</ref> <ref>PMID:15314156</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: Cui JJ]]
-	[[Category: Cui~~, J J~~]]	+	[[Category: Grodsky N]]
-	[[Category: Grodsky, N]]	+	[[Category: McTigue M]]
-	[[Category: McTigue, M]]	+	[[Category: Mroczkowski B]]
-	[[Category: Mroczkowski, B]]	+	[[Category: Ryan K]]
-	[[Category: Ryan, K]]	+	[[Category: Tran-Dube M]]
-	[[Category: Tran-Dube, M]]	+
-	~~[[Category: Atp-binding]]~~	+
-	~~[[Category: C-met]]~~	+
-	~~[[Category: Inhibitor]]~~	+
-	~~[[Category: Kinase]]~~	+
-	~~[[Category: Nucleotide-binding]]~~	+
-	~~[[Category: Transferase]]~~	+
-	~~[[Category: Tyrosine-protein kinase~~]]	+

OCA at 10:54, 7 July 2021

OCA — Wed, 07 Jul 2021 10:54:41 GMT

←Older revision		Revision as of 10:54, 7 July 2021
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	<StructureSection load='2wgj' size='340' side='right'caption='[[2wgj]], [[Resolution\|resolution]] 2.00Å' scene=''>		<StructureSection load='2wgj' size='340' side='right'caption='[[2wgj]], [[Resolution\|resolution]] 2.00Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[2wgj]] 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=2WGJ OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=2WGJ FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[2wgj]] 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=2WGJ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2WGJ 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='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1r1w\|1r1w]], [[1ux3\|1ux3]], [[1fyr\|1fyr]], [[2wd1\|2wd1]], [[2cew\|2cew]], [[1shy\|1shy]], [[2uzx\|2uzx]], [[2uzy\|2uzy]], [[2g15\|2g15]], [[1ssl\|1ssl]], [[1r0p\|1r0p]]</td></tr>	+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[1r1w\|1r1w]], [[1ux3\|1ux3]], [[1fyr\|1fyr]], [[2wd1\|2wd1]], [[2cew\|2cew]], [[1shy\|1shy]], [[2uzx\|2uzx]], [[2uzy\|2uzy]], [[2g15\|2g15]], [[1ssl\|1ssl]], [[1r0p\|1r0p]]</div></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=2wgj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2wgj OCA], [~~http~~://pdbe.org/2wgj PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=2wgj RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/2wgj PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=2wgj 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=2wgj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2wgj OCA], [https://pdbe.org/2wgj PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2wgj RCSB], [https://www.ebi.ac.uk/pdbsum/2wgj PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2wgj ProSAT]</span></td></tr>
	</table>		</table>
	== Evolutionary Conservation ==		== Evolutionary Conservation ==
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	==See Also==		==See Also==
-	*[[Hepatocyte growth factor receptor\|Hepatocyte growth factor receptor]]	+	*[[Hepatocyte growth factor receptor 3D structures\|Hepatocyte growth factor receptor 3D structures]]
	== References ==		== References ==
	<references/>		<references/>

OCA at 12:18, 10 May 2019

OCA — Fri, 10 May 2019 12:18:22 GMT

←Older revision		Revision as of 12:18, 10 May 2019
Line 1:		Line 1:

	==X-ray Structure of PF-02341066 bound to the kinase domain of c-Met==		==X-ray Structure of PF-02341066 bound to the kinase domain of c-Met==
-	<StructureSection load='2wgj' size='340' side='right' caption='[[2wgj]], [[Resolution\|resolution]] 2.00Å' scene=''>	+	<StructureSection load='2wgj' size='340' side='right'caption='[[2wgj]], [[Resolution\|resolution]] 2.00Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[2wgj]] 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=2WGJ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2WGJ FirstGlance]. <br>		<table><tr><td colspan='2'>[[2wgj]] 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=2WGJ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2WGJ 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: Cui, J J]]		[[Category: Cui, J J]]

OCA at 09:14, 26 September 2018

OCA — Wed, 26 Sep 2018 09:14:50 GMT

←Older revision		Revision as of 09:14, 26 September 2018
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-	==X-~~RAY STRUCTURE OF~~ PF-02341066 ~~BOUND TO THE KINASE DOMAIN OF C~~-~~MET~~==	+
		+	==X-ray Structure of PF-02341066 bound to the kinase domain of c-Met==
	<StructureSection load='2wgj' size='340' side='right' caption='[[2wgj]], [[Resolution\|resolution]] 2.00Å' scene=''>		<StructureSection load='2wgj' size='340' side='right' caption='[[2wgj]], [[Resolution\|resolution]] 2.00Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
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	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1r1w\|1r1w]], [[1ux3\|1ux3]], [[1fyr\|1fyr]], [[2wd1\|2wd1]], [[2cew\|2cew]], [[1shy\|1shy]], [[2uzx\|2uzx]], [[2uzy\|2uzy]], [[2g15\|2g15]], [[1ssl\|1ssl]], [[1r0p\|1r0p]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1r1w\|1r1w]], [[1ux3\|1ux3]], [[1fyr\|1fyr]], [[2wd1\|2wd1]], [[2cew\|2cew]], [[1shy\|1shy]], [[2uzx\|2uzx]], [[2uzy\|2uzy]], [[2g15\|2g15]], [[1ssl\|1ssl]], [[1r0p\|1r0p]]</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=2wgj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2wgj OCA], [http://pdbe.org/2wgj PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2wgj RCSB], [http://www.ebi.ac.uk/pdbsum/2wgj 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=2wgj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2wgj OCA], [http://pdbe.org/2wgj PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2wgj RCSB], [http://www.ebi.ac.uk/pdbsum/2wgj PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=2wgj ProSAT]</span></td></tr>
	</table>		</table>
	== Evolutionary Conservation ==		== Evolutionary Conservation ==
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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/wg/2wgj_consurf.spt"</scriptWhenChecked>	+	<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/wg/2wgj_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>
Line 38:		Line 39:
	[[Category: Cui, J J]]		[[Category: Cui, J J]]
	[[Category: Grodsky, N]]		[[Category: Grodsky, N]]
-	[[Category: ~~Mctigue~~, M]]	+	[[Category: McTigue, M]]
	[[Category: Mroczkowski, B]]		[[Category: Mroczkowski, B]]
	[[Category: Ryan, K]]		[[Category: Ryan, K]]

OCA at 04:40, 7 February 2016

OCA — Sun, 07 Feb 2016 04:40:13 GMT

←Older revision		Revision as of 04:40, 7 February 2016
Line 2:		Line 2:
	<StructureSection load='2wgj' size='340' side='right' caption='[[2wgj]], [[Resolution\|resolution]] 2.00Å' scene=''>		<StructureSection load='2wgj' size='340' side='right' caption='[[2wgj]], [[Resolution\|resolution]] 2.00Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[2wgj]] 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=2WGJ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2WGJ FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[2wgj]] 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=2WGJ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2WGJ 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='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1r1w\|1r1w]], [[1ux3\|1ux3]], [[1fyr\|1fyr]], [[2wd1\|2wd1]], [[2cew\|2cew]], [[1shy\|1shy]], [[2uzx\|2uzx]], [[2uzy\|2uzy]], [[2g15\|2g15]], [[1ssl\|1ssl]], [[1r0p\|1r0p]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1r1w\|1r1w]], [[1ux3\|1ux3]], [[1fyr\|1fyr]], [[2wd1\|2wd1]], [[2cew\|2cew]], [[1shy\|1shy]], [[2uzx\|2uzx]], [[2uzy\|2uzy]], [[2g15\|2g15]], [[1ssl\|1ssl]], [[1r0p\|1r0p]]</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=2wgj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2wgj OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2wgj RCSB], [http://www.ebi.ac.uk/pdbsum/2wgj 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=2wgj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2wgj OCA], [http://pdbe.org/2wgj PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2wgj RCSB], [http://www.ebi.ac.uk/pdbsum/2wgj PDBsum]</span></td></tr>
	</table>		</table>
	== Evolutionary Conservation ==		== Evolutionary Conservation ==
Line 16:		Line 16:
	<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=2wgj ConSurf].
	<div style="clear:both"></div>		<div style="clear:both"></div>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
Line 26:		Line 26:
	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 2wgj" style="background-color:#fffaf0;"></div>

	==See Also==		==See Also==
Line 33:		Line 34:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Homo sapiens~~]]	+	[[Category: Human]]
	[[Category: Receptor protein-tyrosine kinase]]		[[Category: Receptor protein-tyrosine kinase]]
	[[Category: Cui, J J]]		[[Category: Cui, J J]]

OCA at 09:17, 20 January 2015

OCA — Tue, 20 Jan 2015 09:17:57 GMT

←Older revision		Revision as of 09:17, 20 January 2015
Line 3:		Line 3:
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[2wgj]] 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=2WGJ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2WGJ FirstGlance]. <br>		<table><tr><td colspan='2'>[[2wgj]] 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=2WGJ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2WGJ FirstGlance]. <br>
-	</td></tr><tr><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><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><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1r1w\|1r1w]], [[1ux3\|1ux3]], [[1fyr\|1fyr]], [[2wd1\|2wd1]], [[2cew\|2cew]], [[1shy\|1shy]], [[2uzx\|2uzx]], [[2uzy\|2uzy]], [[2g15\|2g15]], [[1ssl\|1ssl]], [[1r0p\|1r0p]]</td></tr>	+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1r1w\|1r1w]], [[1ux3\|1ux3]], [[1fyr\|1fyr]], [[2wd1\|2wd1]], [[2cew\|2cew]], [[1shy\|1shy]], [[2uzx\|2uzx]], [[2uzy\|2uzy]], [[2g15\|2g15]], [[1ssl\|1ssl]], [[1r0p\|1r0p]]</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=2wgj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2wgj OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2wgj RCSB], [http://www.ebi.ac.uk/pdbsum/2wgj 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=2wgj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2wgj OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2wgj RCSB], [http://www.ebi.ac.uk/pdbsum/2wgj PDBsum]</span></td></tr>
-	<table>	+	</table>
	== Evolutionary Conservation ==		== Evolutionary Conservation ==
	[[Image:Consurf_key_small.gif\|200px\|right]]		[[Image:Consurf_key_small.gif\|200px\|right]]
Line 35:		Line 35:
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
	[[Category: Receptor protein-tyrosine kinase]]		[[Category: Receptor protein-tyrosine kinase]]
-	[[Category: Cui, J J.]]	+	[[Category: Cui, J J]]
-	[[Category: Grodsky, N.]]	+	[[Category: Grodsky, N]]
-	[[Category: Mctigue, M.]]	+	[[Category: Mctigue, M]]
-	[[Category: Mroczkowski, B.]]	+	[[Category: Mroczkowski, B]]
-	[[Category: Ryan, K.]]	+	[[Category: Ryan, K]]
-	[[Category: Tran-Dube, M.]]	+	[[Category: Tran-Dube, M]]
	[[Category: Atp-binding]]		[[Category: Atp-binding]]
	[[Category: C-met]]		[[Category: C-met]]

OCA at 01:59, 1 October 2014

OCA — Wed, 01 Oct 2014 01:59:57 GMT

←Older revision		Revision as of 01:59, 1 October 2014
Line 1:		Line 1:
-	~~{{STRUCTURE_2wgj\| PDB=2wgj \| SCENE= }}~~	+	==X-RAY STRUCTURE OF PF-02341066 BOUND TO THE KINASE DOMAIN OF C-MET==
-	===X-RAY STRUCTURE OF PF-02341066 BOUND TO THE KINASE DOMAIN OF C-MET===	+	<StructureSection load='2wgj' size='340' side='right' caption='[[2wgj]], [[Resolution\|resolution]] 2.00Å' scene=''>
-	~~{{ABSTRACT_PUBMED_21812414}}~~	+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[2wgj]] 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=2WGJ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2WGJ FirstGlance]. <br>
		+	</td></tr><tr><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><br>
		+	<tr><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1r1w\|1r1w]], [[1ux3\|1ux3]], [[1fyr\|1fyr]], [[2wd1\|2wd1]], [[2cew\|2cew]], [[1shy\|1shy]], [[2uzx\|2uzx]], [[2uzy\|2uzy]], [[2g15\|2g15]], [[1ssl\|1ssl]], [[1r0p\|1r0p]]</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=2wgj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2wgj OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2wgj RCSB], [http://www.ebi.ac.uk/pdbsum/2wgj 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/wg/2wgj_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>
-	~~[[2wgj]] 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=2WGJ OCA].~~	+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>

	==See Also==		==See Also==
	*[[Hepatocyte growth factor receptor\|Hepatocyte growth factor receptor]]		*[[Hepatocyte growth factor receptor\|Hepatocyte growth factor receptor]]
-		+	== References ==
-	==~~Reference~~==	+	<references/>
-	~~<ref group="xtra">PMID:021812414</ref>~~<references ~~group="xtra"~~/><~~references~~/>	+	__TOC__
		+	</StructureSection>
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
	[[Category: Receptor protein-tyrosine kinase]]		[[Category: Receptor protein-tyrosine kinase]]

OCA at 11:06, 24 March 2013

OCA — Sun, 24 Mar 2013 11:06:40 GMT

←Older revision		Revision as of 11:06, 24 March 2013
Line 1:		Line 1:
-	[[Image:2wgj.png\|left\|200px]]
-
-	<!--
-	The line below this paragraph, containing "STRUCTURE_2wgj", 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_2wgj\| PDB=2wgj \| SCENE= }}		{{STRUCTURE_2wgj\| PDB=2wgj \| SCENE= }}
-
	===X-RAY STRUCTURE OF PF-02341066 BOUND TO THE KINASE DOMAIN OF C-MET===		===X-RAY STRUCTURE OF PF-02341066 BOUND TO THE KINASE DOMAIN OF C-MET===
-
-
-	<!--
-	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}}		{{ABSTRACT_PUBMED_21812414}}

	==About this Structure==		==About this Structure==
	[[2wgj]] 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=2WGJ OCA].		[[2wgj]] 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=2WGJ OCA].
		+
		+	==See Also==
		+	*[[Hepatocyte growth factor receptor\|Hepatocyte growth factor receptor]]

	==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 "2wgj" [edit=sysop:move=sysop]

OCA — Wed, 28 Sep 2011 04:56:40 GMT

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

←Older revision

Revision as of 04:56, 28 September 2011

OCA at 04:56, 28 September 2011

OCA — Wed, 28 Sep 2011 04:56:37 GMT

←Older revision		Revision as of 04:56, 28 September 2011
Line 1:		Line 1:
-	{{Seed}}
	[[Image:2wgj.png\|left\|200px]]		[[Image:2wgj.png\|left\|200px]]

Line 12:		Line 11:
	===X-RAY STRUCTURE OF PF-02341066 BOUND TO THE KINASE DOMAIN OF C-MET===		===X-RAY STRUCTURE OF PF-02341066 BOUND TO THE KINASE DOMAIN OF C-MET===

		+
		+	<!--
		+	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==
-	~~2WGJ~~ 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=2WGJ OCA].	+	[[2wgj]] 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=2WGJ 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: Cui, J.]]	+	[[Category: Cui, J J.]]
	[[Category: Grodsky, N.]]		[[Category: Grodsky, N.]]
	[[Category: Mctigue, M.]]		[[Category: Mctigue, M.]]
Line 30:		Line 38:
	[[Category: Transferase]]		[[Category: Transferase]]
	[[Category: Tyrosine-protein kinase]]		[[Category: Tyrosine-protein kinase]]
-
-	''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Sep 1 09:21:46 2010''