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5iu2
From Proteopedia
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| - | '''Unreleased structure''' | ||
| - | + | ==Discovery of imidazoquinolines as a novel class of potent, selective and in vivo efficacious COT kinase inhibitors== | |
| - | + | <StructureSection load='5iu2' size='340' side='right'caption='[[5iu2]], [[Resolution|resolution]] 2.70Å' scene=''> | |
| - | + | == Structural highlights == | |
| - | + | <table><tr><td colspan='2'>[[5iu2]] is a 2 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=5IU2 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5IU2 FirstGlance]. <br> | |
| - | + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.7Å</td></tr> | |
| - | [[Category: | + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=6DA:N-[2-(MORPHOLIN-4-YL)ETHYL]-6-(8-PHENYL-1H-IMIDAZO[4,5-C][1,7]NAPHTHYRIDIN-1-YL)-1,3-BENZOTHIAZOL-2-AMINE'>6DA</scene></td></tr> |
| - | [[Category: Gutmann | + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=5iu2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5iu2 OCA], [https://pdbe.org/5iu2 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5iu2 RCSB], [https://www.ebi.ac.uk/pdbsum/5iu2 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5iu2 ProSAT]</span></td></tr> |
| - | [[Category: Hinniger | + | </table> |
| + | == Function == | ||
| + | [https://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> | ||
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Homo sapiens]] | ||
| + | [[Category: Large Structures]] | ||
| + | [[Category: Gutmann S]] | ||
| + | [[Category: Hinniger A]] | ||
Current revision
Discovery of imidazoquinolines as a novel class of potent, selective and in vivo efficacious COT kinase inhibitors
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