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2oic

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{{STRUCTURE_2oic| PDB=2oic | SCENE= }}
{{STRUCTURE_2oic| PDB=2oic | SCENE= }}
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'''Crystal structure of IRAK4 kinase domain complexed with staurosporine'''
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===Crystal structure of IRAK4 kinase domain complexed with staurosporine===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 17312103 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17312103}}
==Disease==
==Disease==
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[[Category: Villasenor, A G.]]
[[Category: Villasenor, A G.]]
[[Category: Kinase]]
[[Category: Kinase]]
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Revision as of 01:12, 29 July 2008

Image:2oic.png

Template:STRUCTURE 2oic

Contents

Crystal structure of IRAK4 kinase domain complexed with staurosporine

Template:ABSTRACT PUBMED 17312103

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

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