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5cgj

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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.==
==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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<StructureSection load='5cgj' size='340' side='right' caption='[[5cgj]], [[Resolution|resolution]] 3.36&Aring;' scene=''>
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<StructureSection load='5cgj' size='340' side='right'caption='[[5cgj]], [[Resolution|resolution]] 3.36&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<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>
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<table><tr><td colspan='2'>[[5cgj]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Mus_musculus Mus musculus]. 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 [https://proteopedia.org/fgij/fg.htm?mol=5CGJ 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=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>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 3.36&#8491;</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=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>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><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>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=5cgj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5cgj OCA], [https://pdbe.org/5cgj PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5cgj RCSB], [https://www.ebi.ac.uk/pdbsum/5cgj PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5cgj ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
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[[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>
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[https://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>
<div style="background-color:#fffaf0;">
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
== Publication Abstract from PubMed ==
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</div>
</div>
<div class="pdbe-citations 5cgj" style="background-color:#fffaf0;"></div>
<div class="pdbe-citations 5cgj" style="background-color:#fffaf0;"></div>
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==See Also==
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*[[Kelch-like protein 3D structures|Kelch-like protein 3D structures]]
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Engel, C K]]
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[[Category: Large Structures]]
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[[Category: Loenze, P]]
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[[Category: Mus musculus]]
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[[Category: Schimanski-Breves, S]]
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[[Category: Engel CK]]
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[[Category: Beta propeller]]
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[[Category: Loenze P]]
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[[Category: Complex]]
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[[Category: Schimanski-Breves S]]
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[[Category: Inhibitor]]
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[[Category: Protein binding]]
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Current revision

Crystal structure of murine Keap1 in complex with RA839, a non-covalent small-molecule binder to Keap1 and selective activator of Nrf2 signalling.

PDB ID 5cgj

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