2flu

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|ACTIVITY=
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|RELATEDENTRY=[[1u6d|1U6D]], [[1zgk|1ZGK]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2flu FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2flu OCA], [http://www.ebi.ac.uk/pdbsum/2flu PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2flu RCSB]</span>
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[[Category: Lo, J.]]
[[Category: Lo, J.]]
[[Category: beta-propeller]]
[[Category: beta-propeller]]
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[[Category: kelch domain]]
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[[Category: kelch domain,protein-peptide complex]]
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[[Category: protein-peptide complex]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 16:53:58 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:04:37 2008''

Revision as of 00:04, 31 March 2008


PDB ID 2flu

Drag the structure with the mouse to rotate
, resolution 1.50Å
Related: 1U6D, 1ZGK


Resources: FirstGlance, OCA, PDBsum, RCSB
Coordinates: save as pdb, mmCIF, xml



Crystal Structure of the Kelch-Neh2 Complex


Overview

Keap1 is a BTB-Kelch substrate adaptor protein that regulates steady-state levels of Nrf2, a bZIP transcription factor, in response to oxidative stress. We have determined the structure of the Kelch domain of Keap1 bound to a 16-mer peptide from Nrf2 containing a highly conserved DxETGE motif. The Nrf2 peptide contains two short antiparallel beta-strands connected by two overlapping type I beta-turns stabilized by the aspartate and threonine residues. The beta-turn region fits into a binding pocket on the top face of the Kelch domain and the glutamate residues form multiple hydrogen bonds with highly conserved residues in Keap1. Mutagenesis experiments confirmed the role of individual amino acids for binding of Nrf2 to Keap1 and for Keap1-mediated repression of Nrf2-dependent gene expression. Our results provide a detailed picture of how a BTB-Kelch substrate adaptor protein binds to its cognate substrate and will enable the rational design of novel chemopreventive agents.

About this Structure

2FLU is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Structure of the Keap1:Nrf2 interface provides mechanistic insight into Nrf2 signaling., Lo SC, Li X, Henzl MT, Beamer LJ, Hannink M, EMBO J. 2006 Aug 9;25(15):3605-17. Epub 2006 Aug 3. PMID:16888629

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