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2xvd

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{{STRUCTURE_2xvd| PDB=2xvd | SCENE= }}
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==EPHB4 KINASE DOMAIN INHIBITOR COMPLEX==
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===EPHB4 KINASE DOMAIN INHIBITOR COMPLEX===
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<StructureSection load='2xvd' size='340' side='right' caption='[[2xvd]], [[Resolution|resolution]] 1.70&Aring;' scene=''>
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{{ABSTRACT_PUBMED_21441027}}
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== Structural highlights ==
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<table><tr><td colspan='2'>[[2xvd]] 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=2XVD OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2XVD FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=AS6:{4-METHYL-3-[(1-METHYLETHYL)(2-{[3-(METHYLSULFONYL)-5-MORPHOLIN-4-YLPHENYL]AMINO}PYRIMIDIN-4-YL)AMINO]PHENYL}METHANOL'>AS6</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene></td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[2x9f|2x9f]], [[2bba|2bba]], [[2vwu|2vwu]], [[2vx0|2vx0]], [[2vwv|2vwv]], [[2vwz|2vwz]], [[2vwy|2vwy]], [[2vww|2vww]], [[2vwx|2vwx]], [[2vx1|2vx1]]</td></tr>
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<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>
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<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=2xvd FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2xvd OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2xvd RCSB], [http://www.ebi.ac.uk/pdbsum/2xvd PDBsum]</span></td></tr>
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</table>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Optimization of our bis-anilino-pyrimidine series of EphB4 kinase inhibitors led to the discovery of compound 12 which incorporates a key m-hydroxymethylene group on the C4 aniline. 12 displays a good kinase selectivity profile, good physical properties and pharmacokinetic parameters, suggesting it is a suitable candidate to investigate the therapeutic potential of EphB4 kinase inhibitors.
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==Function==
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Inhibitors of the tyrosine kinase EphB4. Part 4: Discovery and optimization of a benzylic alcohol series.,Barlaam B, Ducray R, Lambert-van der Brempt C, Ple P, Bardelle C, Brooks N, Coleman T, Cross D, Kettle JG, Read J Bioorg Med Chem Lett. 2011 Apr 15;21(8):2207-11. PMID:21441027<ref>PMID:21441027</ref>
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[[http://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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==About this Structure==
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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[[2xvd]] 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=2XVD OCA].
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</div>
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==Reference==
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==See Also==
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<ref group="xtra">PMID:021441027</ref><references group="xtra"/><references/>
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*[[Ephrin receptor|Ephrin receptor]]
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== References ==
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<references/>
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__TOC__
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</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Receptor protein-tyrosine kinase]]
[[Category: Receptor protein-tyrosine kinase]]
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[[Category: Brassington, C A.]]
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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: Mccall, E J.]]
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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, A L.]]
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[[Category: Valentine, A L]]
[[Category: Nucleotide-binding]]
[[Category: Nucleotide-binding]]
[[Category: Transferase]]
[[Category: Transferase]]

Revision as of 13:50, 18 December 2014

EPHB4 KINASE DOMAIN INHIBITOR COMPLEX

2xvd, resolution 1.70Å

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