1yhv
From Proteopedia
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| - | [[Image:1yhv.gif|left|200px]] | + | [[Image:1yhv.gif|left|200px]] |
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| - | '''Crystal Structure of PAK1 kinase domain with two point mutations (K299R, T423E)''' | + | {{Structure |
| + | |PDB= 1yhv |SIZE=350|CAPTION= <scene name='initialview01'>1yhv</scene>, resolution 1.80Å | ||
| + | |SITE= | ||
| + | |LIGAND= | ||
| + | |ACTIVITY= [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] | ||
| + | |GENE= PAK1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | ||
| + | }} | ||
| + | |||
| + | '''Crystal Structure of PAK1 kinase domain with two point mutations (K299R, T423E)''' | ||
| + | |||
==Overview== | ==Overview== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1YHV is a [ | + | 1YHV is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1YHV OCA]. |
==Reference== | ==Reference== | ||
| - | The active conformation of the PAK1 kinase domain., Lei M, Robinson MA, Harrison SC, Structure. 2005 May;13(5):769-78. PMID:[http:// | + | The active conformation of the PAK1 kinase domain., Lei M, Robinson MA, Harrison SC, Structure. 2005 May;13(5):769-78. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/15893667 15893667] |
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Non-specific serine/threonine protein kinase]] | [[Category: Non-specific serine/threonine protein kinase]] | ||
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[[Category: kinase; active conformation; activation loop; atp binding site]] | [[Category: kinase; active conformation; activation loop; atp binding site]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 15:23:04 2008'' |
Revision as of 13:23, 20 March 2008
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| , resolution 1.80Å | |||||||
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| Gene: | PAK1 (Homo sapiens) | ||||||
| Activity: | Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Crystal Structure of PAK1 kinase domain with two point mutations (K299R, T423E)
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
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
Page seeded by OCA on Thu Mar 20 15:23:04 2008
