2cdz

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|PDB= 2cdz |SIZE=350|CAPTION= <scene name='initialview01'>2cdz</scene>, resolution 2.30&Aring;
|PDB= 2cdz |SIZE=350|CAPTION= <scene name='initialview01'>2cdz</scene>, resolution 2.30&Aring;
|SITE= <scene name='pdbsite=AC1:23d+Binding+Site+For+Residue+A+1591'>AC1</scene>, <scene name='pdbsite=AC2:So4+Binding+Site+For+Residue+A+1592'>AC2</scene> and <scene name='pdbsite=AC3:So4+Binding+Site+For+Residue+A+1593'>AC3</scene>
|SITE= <scene name='pdbsite=AC1:23d+Binding+Site+For+Residue+A+1591'>AC1</scene>, <scene name='pdbsite=AC2:So4+Binding+Site+For+Residue+A+1592'>AC2</scene> and <scene name='pdbsite=AC3:So4+Binding+Site+For+Residue+A+1593'>AC3</scene>
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|LIGAND= <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene> and <scene name='pdbligand=23D:N2-[(1R,2S)-2-AMINOCYCLOHEXYL]-N6-(3-CHLOROPHENYL)-9-ETHYL-9H-PURINE-2,6-DIAMINE'>23D</scene>
+
|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=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=SEP:PHOSPHOSERINE'>SEP</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>
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|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]
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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>
|GENE=
|GENE=
 +
|DOMAIN=
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|RELATEDENTRY=[[2bva|2BVA]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2cdz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2cdz OCA], [http://www.ebi.ac.uk/pdbsum/2cdz PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2cdz RCSB]</span>
}}
}}
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[[Category: Ugochukwu, E.]]
[[Category: Ugochukwu, E.]]
[[Category: Weigelt, J.]]
[[Category: Weigelt, J.]]
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[[Category: 23D]]
 
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[[Category: CL]]
 
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[[Category: SO4]]
 
[[Category: atp-binding]]
[[Category: atp-binding]]
[[Category: pak4]]
[[Category: pak4]]
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[[Category: transferase]]
[[Category: transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 16:14:11 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 02:20:11 2008''

Revision as of 23:20, 30 March 2008

Image:2cdz.gif


PDB ID 2cdz

Drag the structure with the mouse to rotate
, resolution 2.30Å
Sites: , and
Ligands: , , ,
Activity: Non-specific serine/threonine protein kinase, with EC number 2.7.11.1
Related: 2BVA


Resources: FirstGlance, OCA, PDBsum, RCSB
Coordinates: save as pdb, mmCIF, xml



CRYSTAL STRUCTURE OF THE HUMAN P21-ACTIVATED KINASE 4 IN COMPLEX WITH CGP74514A


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

2CDZ 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

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