1yhw

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[[Image:1yhw.gif|left|200px]]
[[Image:1yhw.gif|left|200px]]
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{{Structure
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|PDB= 1yhw |SIZE=350|CAPTION= <scene name='initialview01'>1yhw</scene>, resolution 1.80&Aring;
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The line below this paragraph, containing "STRUCTURE_1yhw", 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=
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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= PAK1 ([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_1yhw| PDB=1yhw | SCENE= }}
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|RELATEDENTRY=[[1yhv|1YHV]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1yhw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1yhw OCA], [http://www.ebi.ac.uk/pdbsum/1yhw PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1yhw RCSB]</span>
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'''Crystal Structure of PAK1 kinase domain with one point mutations (K299R)'''
'''Crystal Structure of PAK1 kinase domain with one point mutations (K299R)'''
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[[Category: Lei, M.]]
[[Category: Lei, M.]]
[[Category: Robinson, M A.]]
[[Category: Robinson, M A.]]
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[[Category: activation loop]]
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[[Category: Activation loop]]
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[[Category: active conformation]]
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[[Category: Active conformation]]
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[[Category: atp binding site]]
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[[Category: Atp binding site]]
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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 Sat May 3 16:20:17 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 01:07:53 2008''
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Revision as of 13:20, 3 May 2008

Image:1yhw.gif

Template:STRUCTURE 1yhw

Crystal Structure of PAK1 kinase domain with one point mutations (K299R)


Overview

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.

About this Structure

1YHW 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 Page seeded by OCA on Sat May 3 16:20:17 2008

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