4zy3: Difference between revisions

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'''Unreleased structure'''


The entry 4zy3 is ON HOLD  until Paper Publication
==Crystal Structure of Keap1 in Complex with a small chemical compound, K67==
 
<StructureSection load='4zy3' size='340' side='right' caption='[[4zy3]], [[Resolution|resolution]] 1.80&Aring;' scene=''>
Authors: Fukutomi, T., Iso, T., Suzuki, T., Takagi, K., Mizushima, T., Komatsu, M., Yamamoto, M.
== Structural highlights ==
 
<table><tr><td colspan='2'>[[4zy3]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4ZY3 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4ZY3 FirstGlance]. <br>
Description: Crystal Structure of Keap1 in Complex with a small chemical compound, K67
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=FMT:FORMIC+ACID'>FMT</scene>, <scene name='pdbligand=K67:N,N-[2-(2-OXOPROPYL)NAPHTHALENE-1,4-DIYL]BIS(4-ETHOXYBENZENESULFONAMIDE)'>K67</scene></td></tr>
[[Category: Unreleased Structures]]
<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=4zy3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4zy3 OCA], [http://pdbe.org/4zy3 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4zy3 RCSB], [http://www.ebi.ac.uk/pdbsum/4zy3 PDBsum]</span></td></tr>
</table>
== 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: Fukutomi, T]]
[[Category: Iso, T]]
[[Category: Iso, T]]
[[Category: Yamamoto, M]]
[[Category: Fukutomi, T]]
[[Category: Komatsu, M]]
[[Category: Komatsu, M]]
[[Category: Mizushima, T]]
[[Category: Mizushima, T]]
[[Category: Suzuki, T]]
[[Category: Suzuki, T]]
[[Category: Takagi, K]]
[[Category: Takagi, K]]
[[Category: Yamamoto, M]]
[[Category: Double glycine repeat]]
[[Category: Keap1]]
[[Category: Kelch domain]]
[[Category: Nrf2]]
[[Category: P62]]
[[Category: Small molecule binding]]
[[Category: Stress sensor]]
[[Category: Transcription]]

Revision as of 01:52, 2 June 2016

Crystal Structure of Keap1 in Complex with a small chemical compound, K67Crystal Structure of Keap1 in Complex with a small chemical compound, K67

Structural highlights

4zy3 is a 2 chain structure. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:,
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum

Function

[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).[1] [2]

References

  1. ↑ Itoh K, Wakabayashi N, Katoh Y, Ishii T, Igarashi K, Engel JD, Yamamoto M. Keap1 represses nuclear activation of antioxidant responsive elements by Nrf2 through binding to the amino-terminal Neh2 domain. Genes Dev. 1999 Jan 1;13(1):76-86. PMID:9887101
  2. ↑ McMahon M, Itoh K, Yamamoto M, Hayes JD. Keap1-dependent proteasomal degradation of transcription factor Nrf2 contributes to the negative regulation of antioxidant response element-driven gene expression. J Biol Chem. 2003 Jun 13;278(24):21592-600. Epub 2003 Apr 7. PMID:12682069 doi:10.1074/jbc.M300931200

4zy3, resolution 1.80Å

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OCA
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