3wzu

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'''Unreleased structure'''
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==THE STRUCTURE OF MAP2K7 IN COMPLEX WITH 5Z-7-oxozeaenol==
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<StructureSection load='3wzu' size='340' side='right' caption='[[3wzu]], [[Resolution|resolution]] 3.01&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[3wzu]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3WZU OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3WZU 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=1FM:(3S,5Z,8S,9S,11E)-8,9,16-TRIHYDROXY-14-METHOXY-3-METHYL-3,4,9,10-TETRAHYDRO-1H-2-BENZOXACYCLOTETRADECINE-1,7(8H)-DIONE'>1FM</scene></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/Mitogen-activated_protein_kinase_kinase Mitogen-activated protein kinase kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.12.2 2.7.12.2] </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=3wzu FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3wzu OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3wzu RCSB], [http://www.ebi.ac.uk/pdbsum/3wzu PDBsum]</span></td></tr>
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</table>
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== Function ==
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[[http://www.uniprot.org/uniprot/MP2K7_HUMAN MP2K7_HUMAN]] Dual specificity protein kinase which acts as an essential component of the MAP kinase signal transduction pathway. Essential component of the stress-activated protein kinase/c-Jun N-terminal kinase (SAP/JNK) signaling pathway. With MAP2K4/MKK4, is the one of the only known kinase to directly activate the stress-activated protein kinase/c-Jun N-terminal kinases MAPK8/JNK1, MAPK9/JNK2 and MAPK10/JNK3. MAP2K4/MKK4 and MAP2K7/MKK7 both activate the JNKs by phosphorylation, but they differ in their preference for the phosphorylation site in the Thr-Pro-Tyr motif. MAP2K4/MKK4 shows preference for phosphorylation of the Tyr residue and MAP2K7/MKK7 for the Thr residue. The monophosphorylation of JNKs on the Thr residue is sufficient to increase JNK activity indicating that MAP2K7/MKK7 is important to trigger JNK activity, while the additional phosphorylation of the Tyr residue by MAP2K4/MKK4 ensures optimal JNK activation. Has a specific role in JNK signal transduction pathway activated by proinflammatory cytokines. The MKK/JNK signaling pathway is also involved in mitochondrial death signaling pathway, including the release cytochrome c, leading to apoptosis.<ref>PMID:9372971</ref> <ref>PMID:9312068</ref> <ref>PMID:9535930</ref> [:]
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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5Z-7-Oxozeaenol (5Z7O) is a covalent bonding inhibitor against the several protein kinases (e.g., ERK2 and TAK1) that possess a free cysteine at the gatekeeper-2 position. In addition to this cysteine, MAP2K7 has three other cysteine residues that are candidate for covalent bonding by the inhibitor 5Z7O. The crystal structure of the MAP2K7/5Z7O complex revealed that the inhibitor binds to MAP2K7 at a cysteine residue located at the end of the hinge region and not at the gatekeeper-2 residue. The structural insights into the interaction of 5Z7O with MAP2K7 should aid the development of 5Z7O derivatives with improved potency and selectivity.
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The entry 3wzu is ON HOLD until Paper Publication
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5Z-7-Oxozeaenol covalently binds to MAP2K7 at Cys218 in an unprecedented manner.,Sogabe Y, Matsumoto T, Hashimoto T, Kirii Y, Sawa M, Kinoshita T Bioorg Med Chem Lett. 2014 Dec 13. pii: S0960-894X(14)01308-0. doi:, 10.1016/j.bmcl.2014.12.011. PMID:25529738<ref>PMID:25529738</ref>
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Authors: Sogabe, Y., Hashimoto, Y., Matsumoto, T., Kinoshita, T.
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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Description: THE STRUCTURE OF MAP2K7 IN COMPLEX WITH 5Z-7-oxozeaenol
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== References ==
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[[Category: Unreleased Structures]]
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<references/>
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__TOC__
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</StructureSection>
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[[Category: Mitogen-activated protein kinase kinase]]
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[[Category: Hashimoto, Y]]
[[Category: Kinoshita, T]]
[[Category: Kinoshita, T]]
[[Category: Matsumoto, T]]
[[Category: Matsumoto, T]]
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[[Category: Hashimoto, Y]]
 
[[Category: Sogabe, Y]]
[[Category: Sogabe, Y]]
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[[Category: Protein kinase]]
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[[Category: Transferase-transferase inhibitor complex]]

Revision as of 13:28, 14 January 2015

THE STRUCTURE OF MAP2K7 IN COMPLEX WITH 5Z-7-oxozeaenol

3wzu, resolution 3.01Å

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