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4y83

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'''Unreleased structure'''
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==Crystal structure of COT kinase domain in complex with 5-(2-amino-5-(quinolin-3-yl)pyridin-3-yl)-1,3,4-oxadiazole-2(3H)-thione==
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<StructureSection load='4y83' size='340' side='right' caption='[[4y83]], [[Resolution|resolution]] 2.89&Aring;' scene=''>
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The entry 4y83 is ON HOLD
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4y83]] is a 3 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4Y83 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4Y83 FirstGlance]. <br>
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Authors: Gutmann, S., Hinniger, A.
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=49B:5-[2-AMINO-5-(QUINOLIN-3-YL)PYRIDIN-3-YL]-1,3,4-OXADIAZOLE-2(3H)-THIONE'>49B</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_kinase Mitogen-activated protein kinase kinase kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.25 2.7.11.25] </span></td></tr>
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Description: Crystal structure of COT kinase domain in complex with 5-(2-amino-5-(quinolin-3-yl)pyridin-3-yl)-1,3,4-oxadiazole-2(3H)-thione
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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=4y83 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4y83 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4y83 RCSB], [http://www.ebi.ac.uk/pdbsum/4y83 PDBsum]</span></td></tr>
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[[Category: Unreleased Structures]]
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</table>
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== Function ==
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[[http://www.uniprot.org/uniprot/M3K8_HUMAN M3K8_HUMAN]] Required for lipopolysaccharide (LPS)-induced, TLR4-mediated activation of the MAPK/ERK pathway in macrophages, thus being critical for production of the proinflammatory cytokine TNF-alpha (TNF) during immune responses. Involved in the regulation of T-helper cell differentiation and IFNG expression in T-cells. Involved in mediating host resistance to bacterial infection through negative regulation of type I interferon (IFN) production. In vitro, activates MAPK/ERK pathway in response to IL1 in an IRAK1-independent manner, leading to up-regulation of IL8 and CCL4. Transduces CD40 and TNFRSF1A signals that activate ERK in B-cells and macrophages, and thus may play a role in the regulation of immunoglobulin production. May also play a role in the transduction of TNF signals that activate JNK and NF-kappa-B in some cell types. In adipocytes, activates MAPK/ERK pathway in an IKBKB-dependent manner in response to IL1B and TNF, but not insulin, leading to induction of lipolysis. Plays a role in the cell cycle. Isoform 1 shows some transforming activity, although it is much weaker than that of the activated oncogenic variant.<ref>PMID:11342626</ref> <ref>PMID:12667451</ref> <ref>PMID:15169888</ref> <ref>PMID:16371247</ref> <ref>PMID:1833717</ref> <ref>PMID:19001140</ref> <ref>PMID:19754427</ref> <ref>PMID:19808894</ref>
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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 kinase]]
[[Category: Gutmann, S]]
[[Category: Gutmann, S]]
[[Category: Hinniger, A]]
[[Category: Hinniger, A]]
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[[Category: Complex]]
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[[Category: Cot]]
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[[Category: Inhibitor]]
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[[Category: Kinase]]
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[[Category: Map3k8]]
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[[Category: Tpl-2]]
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[[Category: Transferase]]

Revision as of 13:03, 6 May 2015

Crystal structure of COT kinase domain in complex with 5-(2-amino-5-(quinolin-3-yl)pyridin-3-yl)-1,3,4-oxadiazole-2(3H)-thione

4y83, resolution 2.89Å

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