2f57

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[[Image:2f57.gif|left|200px]]
[[Image:2f57.gif|left|200px]]
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{{Structure
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|PDB= 2f57 |SIZE=350|CAPTION= <scene name='initialview01'>2f57</scene>, resolution 1.80&Aring;
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The line below this paragraph, containing "STRUCTURE_2f57", creates the "Structure Box" on the page.
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|SITE=
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|LIGAND= <scene name='pdbligand=23D:N2-[(1R,2S)-2-AMINOCYCLOHEXYL]-N6-(3-CHLOROPHENYL)-9-ETHYL-9H-PURINE-2,6-DIAMINE'>23D</scene>, <scene name='pdbligand=SEP:PHOSPHOSERINE'>SEP</scene>, <scene name='pdbligand=TRS:2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL'>TRS</scene>
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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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{{STRUCTURE_2f57| PDB=2f57 | SCENE= }}
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2f57 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2f57 OCA], [http://www.ebi.ac.uk/pdbsum/2f57 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2f57 RCSB]</span>
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'''Crystal Structure Of The Human P21-Activated Kinase 5'''
'''Crystal Structure Of The Human P21-Activated Kinase 5'''
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[[Category: Ugochukwu, E.]]
[[Category: Ugochukwu, E.]]
[[Category: Weigelt, J.]]
[[Category: Weigelt, J.]]
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[[Category: groupii pak]]
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[[Category: Groupii pak]]
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[[Category: kinase domain]]
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[[Category: Kinase domain]]
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[[Category: pak5]]
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[[Category: Pak5]]
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[[Category: sgc]]
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[[Category: Sgc]]
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[[Category: structural genomic]]
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[[Category: Structural genomic]]
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[[Category: structural genomics consortium]]
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[[Category: Structural genomics consortium]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 03:28:28 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 02:58:04 2008''
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Revision as of 00:28, 4 May 2008

Template:STRUCTURE 2f57

Crystal Structure Of The Human P21-Activated Kinase 5


Overview

p21-activated kinases have been classified into two groups based on their domain architecture. Group II PAKs (PAK4-6) regulate a wide variety of cellular functions, and PAK deregulation has been linked to tumor development. Structural comparison of five high-resolution structures comprising all active, monophosphorylated group II catalytic domains revealed a surprising degree of domain plasticity, including a number of catalytically productive and nonproductive conformers. Rearrangements of helix alphaC, a key regulatory element of kinase function, resulted in an additional helical turn at the alphaC N terminus and a distortion of its C terminus, a movement hitherto unseen in protein kinases. The observed structural changes led to the formation of interactions between conserved residues that structurally link the glycine-rich loop, alphaC, and the activation segment and firmly anchor alphaC in an active conformation. Inhibitor screening identified six potent PAK inhibitors from which a tri-substituted purine inhibitor was cocrystallized with PAK4 and PAK5.

About this Structure

2F57 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Crystal Structures of the p21-activated kinases PAK4, PAK5, and PAK6 reveal catalytic domain plasticity of active group II PAKs., Eswaran J, Lee WH, Debreczeni JE, Filippakopoulos P, Turnbull A, Fedorov O, Deacon SW, Peterson JR, Knapp S, Structure. 2007 Feb;15(2):201-13. PMID:17292838 Page seeded by OCA on Sun May 4 03:28:28 2008

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