1yhv

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[[Image:1yhv.gif|left|200px]]
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{{Seed}}
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[[Image:1yhv.png|left|200px]]
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{{STRUCTURE_1yhv| PDB=1yhv | SCENE= }}
{{STRUCTURE_1yhv| PDB=1yhv | SCENE= }}
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'''Crystal Structure of PAK1 kinase domain with two point mutations (K299R, T423E)'''
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===Crystal Structure of PAK1 kinase domain with two point mutations (K299R, T423E)===
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==Overview==
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The p21-activated kinases (PAKs) participate in cytoskeletal control networks, downstream of Rho-family GTPases. A structure of PAK1 in an autoregulated, "off" state showed that a regulatory region, N-terminal to the kinase domain, forces the latter into an inactive conformation, prevents phosphorylation of Thr423 in the activation loop, and promotes dimerization. We have now determined structures at 1.8 A resolution for the free PAK1 kinase domain, with a mutation in the active site that blocks enzymatic activity, and for the same domain with a "phosphomimetic" mutation in the activation loop. The two very similar structures show that even in the absence of a phosphorylated Thr423, the kinase has an essentially active conformation. When Cdc42 binds the regulatory region and dissociates the dimer, PAK1 will be in an "intermediate-active" state, with a capacity to phosphorylate itself or other substrates even prior to modification of its activation loop.
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The line below this paragraph, {{ABSTRACT_PUBMED_15893667}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 15893667 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15893667}}
==About this Structure==
==About this Structure==
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[[Category: Atp binding site]]
[[Category: Atp binding site]]
[[Category: Kinase]]
[[Category: Kinase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 16:20:14 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 06:06:58 2008''

Revision as of 03:07, 29 July 2008

Image:1yhv.png

Template:STRUCTURE 1yhv

Crystal Structure of PAK1 kinase domain with two point mutations (K299R, T423E)

Template:ABSTRACT PUBMED 15893667

About this Structure

1YHV is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

The active conformation of the PAK1 kinase domain., Lei M, Robinson MA, Harrison SC, Structure. 2005 May;13(5):769-78. PMID:15893667

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