2clq

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{{STRUCTURE_2clq| PDB=2clq | SCENE= }}
{{STRUCTURE_2clq| PDB=2clq | SCENE= }}
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'''STRUCTURE OF MITOGEN-ACTIVATED PROTEIN KINASE KINASE KINASE 5'''
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===STRUCTURE OF MITOGEN-ACTIVATED PROTEIN KINASE KINASE KINASE 5===
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==Overview==
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Apoptosis signal-regulating kinase 1 (ASK1) plays an essential role in stress and immune response and has been linked to the development of several diseases. Here, we present the structure of the human ASK1 catalytic domain in complex with staurosporine. Analytical ultracentrifugation (AUC) and crystallographic analysis showed that ASK1 forms a tight dimer (K(d) approximately 0.2 microM) interacting in a head-to-tail fashion. We found that the ASK1 phosphorylation motifs differ from known ASK1 phosphorylation sites but correspond well to autophosphorylation sites identified by mass spectrometry. Reporter gene assays showed that all three identified in vitro autophosphorylation sites (Thr813, Thr838, Thr842) regulate ASK1 signaling, but site-directed mutants showed catalytic activities similar to wild-type ASK1, suggesting a regulatory mechanism independent of ASK1 kinase activity. The determined high-resolution structure of ASK1 and identified ATP mimetic inhibitors will provide a first starting point for the further development of selective inhibitors.
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(as it appears on PubMed at http://www.pubmed.gov), where 17937911 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17937911}}
==About this Structure==
==About this Structure==
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[[Category: Serine/threonine-protein kinase]]
[[Category: Serine/threonine-protein kinase]]
[[Category: Transferase]]
[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 22:26:42 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 21:19:51 2008''

Revision as of 18:19, 28 July 2008

Image:2clq.png

Template:STRUCTURE 2clq

STRUCTURE OF MITOGEN-ACTIVATED PROTEIN KINASE KINASE KINASE 5

Template:ABSTRACT PUBMED 17937911

About this Structure

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

Reference

Structural and functional characterization of the human protein kinase ASK1., Bunkoczi G, Salah E, Filippakopoulos P, Fedorov O, Muller S, Sobott F, Parker SA, Zhang H, Min W, Turk BE, Knapp S, Structure. 2007 Oct;15(10):1215-26. PMID:17937911

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