2vx0

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Current revision (15:35, 13 December 2023) (edit) (undo)
 
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<StructureSection load='2vx0' size='340' side='right'caption='[[2vx0]], [[Resolution|resolution]] 2.10&Aring;' scene=''>
<StructureSection load='2vx0' size='340' side='right'caption='[[2vx0]], [[Resolution|resolution]] 2.10&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[2vx0]] 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=2VX0 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2VX0 FirstGlance]. <br>
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<table><tr><td colspan='2'>[[2vx0]] 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=2VX0 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2VX0 FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=7X7:N-(5-CHLORO-1,3-BENZODIOXOL-4-YL)-N-(3-MORPHOLIN-4-YLPHENYL)PYRIMIDINE-2,4-DIAMINE'>7X7</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene></td></tr>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.1&#8491;</td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[2bba|2bba]], [[2vwu|2vwu]], [[2vwv|2vwv]], [[2vwy|2vwy]], [[2vww|2vww]], [[2vwx|2vwx]], [[2vwz|2vwz]], [[2vx1|2vx1]]</div></td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=7X7:N-(5-CHLORO-1,3-BENZODIOXOL-4-YL)-N-(3-MORPHOLIN-4-YLPHENYL)PYRIMIDINE-2,4-DIAMINE'>7X7</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene></td></tr>
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<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>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=2vx0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2vx0 OCA], [https://pdbe.org/2vx0 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2vx0 RCSB], [https://www.ebi.ac.uk/pdbsum/2vx0 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2vx0 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=2vx0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2vx0 OCA], [https://pdbe.org/2vx0 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2vx0 RCSB], [https://www.ebi.ac.uk/pdbsum/2vx0 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2vx0 ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
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[[https://www.uniprot.org/uniprot/EPHB4_HUMAN EPHB4_HUMAN]] Receptor tyrosine kinase which binds promiscuously transmembrane ephrin-B family ligands residing on adjacent cells, leading to contact-dependent bidirectional signaling into neighboring cells. The signaling pathway downstream of the receptor is referred to as forward signaling while the signaling pathway downstream of the ephrin ligand is referred to as reverse signaling. Together with its cognate ligand/functional ligand EFNB2 plays a central role in heart morphogenesis and angiogenesis through regulation of cell adhesion and cell migration. EPHB4-mediated forward signaling controls cellular repulsion and segregation form EFNB2-expressing cells. Plays also a role in postnatal blood vessel remodeling, morphogenesis and permeability and is thus important in the context of tumor angiogenesis.<ref>PMID:12734395</ref> <ref>PMID:16424904</ref>
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[https://www.uniprot.org/uniprot/EPHB4_HUMAN EPHB4_HUMAN] Receptor tyrosine kinase which binds promiscuously transmembrane ephrin-B family ligands residing on adjacent cells, leading to contact-dependent bidirectional signaling into neighboring cells. The signaling pathway downstream of the receptor is referred to as forward signaling while the signaling pathway downstream of the ephrin ligand is referred to as reverse signaling. Together with its cognate ligand/functional ligand EFNB2 plays a central role in heart morphogenesis and angiogenesis through regulation of cell adhesion and cell migration. EPHB4-mediated forward signaling controls cellular repulsion and segregation form EFNB2-expressing cells. Plays also a role in postnatal blood vessel remodeling, morphogenesis and permeability and is thus important in the context of tumor angiogenesis.<ref>PMID:12734395</ref> <ref>PMID:16424904</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>
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[[Category: Human]]
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[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Large Structures]]
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[[Category: Receptor protein-tyrosine kinase]]
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[[Category: Barratt D]]
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[[Category: Barratt, D]]
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[[Category: Brassington CA]]
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[[Category: Brassington, C A]]
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[[Category: Green I]]
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[[Category: Green, I]]
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[[Category: Kettle JG]]
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[[Category: Kettle, J G]]
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[[Category: Leach AG]]
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[[Category: Leach, A G]]
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[[Category: McCall EJ]]
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[[Category: McCall, E J]]
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[[Category: Read J]]
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[[Category: Read, J]]
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[[Category: Valentine AL]]
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[[Category: Valentine, A L]]
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[[Category: Atp-binding]]
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[[Category: Glycoprotein]]
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[[Category: Membrane]]
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[[Category: Mutant]]
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[[Category: Nucleotide-binding]]
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[[Category: Phosphoprotein]]
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[[Category: Polymorphism]]
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[[Category: Transferase]]
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[[Category: Transmembrane]]
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[[Category: Unphosphorylated]]
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Current revision

ephB4 kinase domain inhibitor complex

PDB ID 2vx0

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