2oic

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[[Image:2oic.gif|left|200px]]
[[Image:2oic.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2oic |SIZE=350|CAPTION= <scene name='initialview01'>2oic</scene>, resolution 2.40&Aring;
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The line below this paragraph, containing "STRUCTURE_2oic", 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=STU:STAUROSPORINE'>STU</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_2oic| PDB=2oic | SCENE= }}
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|RELATEDENTRY=[[2oib|2OIB]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2oic FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2oic OCA], [http://www.ebi.ac.uk/pdbsum/2oic PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2oic RCSB]</span>
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}}
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'''Crystal structure of IRAK4 kinase domain complexed with staurosporine'''
'''Crystal structure of IRAK4 kinase domain complexed with staurosporine'''
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[[Category: Kuglstatter, A.]]
[[Category: Kuglstatter, A.]]
[[Category: Villasenor, A G.]]
[[Category: Villasenor, A G.]]
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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 10:58:55 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:18:16 2008''
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Revision as of 07:58, 4 May 2008

Image:2oic.gif

Template:STRUCTURE 2oic

Crystal structure of IRAK4 kinase domain complexed with staurosporine


Contents

Overview

IL-1R-associated kinase (IRAK)4 plays a central role in innate and adaptive immunity, and is a crucial component in IL-1/TLR signaling. We have determined the crystal structures of the apo and ligand-bound forms of human IRAK4 kinase domain. These structures reveal several features that provide opportunities for the design of selective IRAK4 inhibitors. The N-terminal lobe of the IRAK4 kinase domain is structurally distinctive due to a loop insertion after an extended N-terminal helix. The gatekeeper residue is a tyrosine, a unique feature of the IRAK family. The IRAK4 structures also provide insights into the regulation of its activity. In the apo structure, two conformations coexist, differing in the relative orientation of the two kinase lobes and the position of helix C. In the presence of an ATP analog only one conformation is observed, indicating that this is the active conformation.

Disease

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

About this Structure

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

Reference

Cutting Edge: IL-1 receptor-associated kinase 4 structures reveal novel features and multiple conformations., Kuglstatter A, Villasenor AG, Shaw D, Lee SW, Tsing S, Niu L, Song KW, Barnett JW, Browner MF, J Immunol. 2007 Mar 1;178(5):2641-5. PMID:17312103 Page seeded by OCA on Sun May 4 10:58:55 2008

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OCA

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