6ib2

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'''Unreleased structure'''
 
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The entry 6ib2 is ON HOLD until Paper Publication
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==The structure of MKK7 in complex with the covalent 4-amino-pyrazolopyrimidine 4a==
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<StructureSection load='6ib2' size='340' side='right' caption='[[6ib2]], [[Resolution|resolution]] 2.10&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[6ib2]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6IB2 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6IB2 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=862:1-[(3~{R})-3-[4-azanyl-3-[1-(4-ethanoylphenyl)-1,2,3-triazol-4-yl]pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]propan-1-one'>862</scene></td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[6ib0|6ib0]]</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=6ib2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6ib2 OCA], [http://pdbe.org/6ib2 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6ib2 RCSB], [http://www.ebi.ac.uk/pdbsum/6ib2 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6ib2 ProSAT]</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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The protein kinase MKK7 is linked to neuronal development and the onset of cancer. The field, however, lacks high-quality functional probes that would allow for the dissection of its detailed functions. Against this background, we describe an effective covalent inhibitor of MKK7 based on the pyrazolopyrimidine scaffold.
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Authors: Wolle, P., Hardick, J., Mueller, M.P., Rauh, D.
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Targeting the MKK7-JNK (Mitogen-Activated Protein Kinase Kinase 7-c-Jun N-Terminal Kinase) Pathway with Covalent Inhibitors.,Wolle P, Hardick J, Cronin SJF, Engel J, Baumann M, Lategahn J, Penninger JM, Rauh D J Med Chem. 2019 Feb 21. doi: 10.1021/acs.jmedchem.9b00102. PMID:30768270<ref>PMID:30768270</ref>
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Description: The structure of MKK7 in complex with the covalent 4-amino-pyrazolopyrimidine 3a
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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[[Category: Unreleased Structures]]
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</div>
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<div class="pdbe-citations 6ib2" style="background-color:#fffaf0;"></div>
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== References ==
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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]]
[[Category: Hardick, J]]
[[Category: Hardick, J]]
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[[Category: Wolle, P]]
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[[Category: Mueller, M P]]
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[[Category: Mueller, M.P]]
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[[Category: Rauh, D]]
[[Category: Rauh, D]]
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[[Category: Wolle, P]]
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[[Category: Covalent]]
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[[Category: Inhibitor]]
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[[Category: Jnk]]
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[[Category: Kinase]]
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[[Category: Mkk7]]
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[[Category: Transferase]]

Revision as of 15:25, 27 February 2019

The structure of MKK7 in complex with the covalent 4-amino-pyrazolopyrimidine 4a

6ib2, resolution 2.10Å

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