2nru

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[[Image:2nru.jpg|left|200px]]
[[Image:2nru.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2nru |SIZE=350|CAPTION= <scene name='initialview01'>2nru</scene>, resolution 2.00&Aring;
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The line below this paragraph, containing "STRUCTURE_2nru", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=SEP:PHOSPHOSERINE'>SEP</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=T12:1-(3-HYDROXYPROPYL)-2-[(3-NITROBENZOYL)AMINO]-1H-BENZIMIDAZOL-5-YL+PIVALATE'>T12</scene>, <scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= IRAK4 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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|DOMAIN=
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{{STRUCTURE_2nru| PDB=2nru | SCENE= }}
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|RELATEDENTRY=[[2nry|2NRY]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2nru FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2nru OCA], [http://www.ebi.ac.uk/pdbsum/2nru PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2nru RCSB]</span>
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}}
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'''Crystal structure of IRAK-4'''
'''Crystal structure of IRAK-4'''
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[[Category: Walker, N P.C.]]
[[Category: Walker, N P.C.]]
[[Category: Wang, Z.]]
[[Category: Wang, Z.]]
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[[Category: inhibitor]]
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[[Category: Inhibitor]]
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[[Category: irak]]
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[[Category: Irak]]
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[[Category: kinase]]
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[[Category: Kinase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 09:50:00 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:07:24 2008''
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Revision as of 06:50, 4 May 2008

Image:2nru.jpg

Template:STRUCTURE 2nru

Crystal structure of IRAK-4


Contents

Overview

Interleukin-1 (IL-1) receptor-associated kinase-4 (IRAK-4) is a serine/threonine kinase that plays an essential role in signal transduction by Toll/IL-1 receptors (TIRs). Here, we report the crystal structures of the phosphorylated human IRAK-4 kinase domain in complex with a potent inhibitor and with staurosporine to 2.0 and 2.2 A, respectively. The structures reveal that IRAK-4 has a unique tyrosine gatekeeper residue that interacts with the conserved glutamate from helix alphaC. Consequently, helix alphaC is "pulled in" to maintain the active orientation, and the usual pre-existing hydrophobic back pocket of the ATP-binding site is abolished. The peptide substrate-binding site is more open when compared with other protein kinases due to a marked movement of helix alphaG. The pattern of phosphate ligand interactions in the activation loop bears a close resemblance to that of a tyrosine kinase. Our results provide insights into IRAK-4 function and the design of selective inhibitors.

Disease

Known disease associated with this structure: IRAK4 deficiency OMIM:[606883], Invasive pneumococcal disease, recurrent isolated, 1 OMIM:[606883]

About this Structure

2NRU is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Crystal structures of IRAK-4 kinase in complex with inhibitors: a serine/threonine kinase with tyrosine as a gatekeeper., Wang Z, Liu J, Sudom A, Ayres M, Li S, Wesche H, Powers JP, Walker NP, Structure. 2006 Dec;14(12):1835-44. PMID:17161373 Page seeded by OCA on Sun May 4 09:50:00 2008

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