5cgj: Difference between revisions
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''' | ==Crystal structure of murine Keap1 in complex with RA839, a non-covalent small-molecule binder to Keap1 and selective activator of Nrf2 signalling.== | ||
<StructureSection load='5cgj' size='340' side='right' caption='[[5cgj]], [[Resolution|resolution]] 3.36Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[5cgj]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5CGJ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5CGJ FirstGlance]. <br> | |||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=51M:(3S)-1-(4-{[(2,3,5,6-TETRAMETHYLPHENYL)SULFONYL]AMINO}NAPHTHALEN-1-YL)PYRROLIDINE-3-CARBOXYLIC+ACID'>51M</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr> | |||
<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=5cgj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5cgj OCA], [http://pdbe.org/5cgj PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5cgj RCSB], [http://www.ebi.ac.uk/pdbsum/5cgj PDBsum]</span></td></tr> | |||
</table> | |||
[[Category: | == Function == | ||
[[http://www.uniprot.org/uniprot/KEAP1_MOUSE KEAP1_MOUSE]] Retains NFE2L2/NRF2 in the cytosol. Functions as substrate adapter protein for the E3 ubiquitin ligase complex formed by CUL3 and RBX1. Targets NFE2L2/NRF2 for ubiquitination and degradation by the proteasome, thus resulting in the suppression of its transcriptional activity and the repression of antioxidant response element-mediated detoxifying enzyme gene expression. May also retain BPTF in the cytosol. Targets PGAM5 for ubiquitination and degradation by the proteasome (By similarity).<ref>PMID:9887101</ref> <ref>PMID:12682069</ref> | |||
== References == | |||
<references/> | |||
__TOC__ | |||
</StructureSection> | |||
[[Category: Engel, C K]] | |||
[[Category: Loenze, P]] | [[Category: Loenze, P]] | ||
[[Category: Schimanski-Breves, S]] | [[Category: Schimanski-Breves, S]] | ||
[[Category: Beta propeller]] | |||
[[Category: Complex]] | |||
[[Category: Inhibitor]] | |||
[[Category: Protein binding]] | |||
Revision as of 05:33, 22 October 2015
Crystal structure of murine Keap1 in complex with RA839, a non-covalent small-molecule binder to Keap1 and selective activator of Nrf2 signalling.
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