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2biy

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[[Image:2biy.gif|left|200px]]
[[Image:2biy.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2biy |SIZE=350|CAPTION= <scene name='initialview01'>2biy</scene>, resolution 1.95&Aring;
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The line below this paragraph, containing "STRUCTURE_2biy", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=BC6:Atp+Binding+Site+For+Chain+A'>BC6</scene>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=ATP:ADENOSINE-5&#39;-TRIPHOSPHATE'>ATP</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</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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or leave the SCENE parameter empty for the default display.
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|GENE=
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|DOMAIN=
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{{STRUCTURE_2biy| PDB=2biy | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2biy FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2biy OCA], [http://www.ebi.ac.uk/pdbsum/2biy PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2biy RCSB]</span>
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}}
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'''STRUCTURE OF PDK1-S241A MUTANT KINASE DOMAIN'''
'''STRUCTURE OF PDK1-S241A MUTANT KINASE DOMAIN'''
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[[Category: Komander, D.]]
[[Category: Komander, D.]]
[[Category: Kular, G S.]]
[[Category: Kular, G S.]]
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[[Category: ac-helix]]
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[[Category: Ac-helix]]
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[[Category: agc kinase]]
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[[Category: Agc kinase]]
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[[Category: atp-binding]]
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[[Category: Atp-binding]]
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[[Category: phosphoinositide dependent protein kinase]]
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[[Category: Phosphoinositide dependent protein kinase]]
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[[Category: phosphorylation]]
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[[Category: Phosphorylation]]
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[[Category: pi3-kinase signalling]]
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[[Category: Pi3-kinase signalling]]
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[[Category: pif-pocket]]
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[[Category: Pif-pocket]]
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[[Category: pka]]
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[[Category: Pka]]
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[[Category: pkb]]
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[[Category: Pkb]]
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[[Category: serine-threonine-protein kinase]]
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[[Category: Serine-threonine-protein kinase]]
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[[Category: t-loop mutant]]
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[[Category: T-loop mutant]]
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[[Category: transferase]]
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[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 20:21:20 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 02:07:08 2008''
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Revision as of 17:21, 3 May 2008

Image:2biy.gif

Template:STRUCTURE 2biy

STRUCTURE OF PDK1-S241A MUTANT KINASE DOMAIN


Overview

3-Phosphoinositide-dependent protein kinase-1 (PDK1) phosphorylates the T-loop of several AGC (cAMP-dependent, cGMP-dependent, protein kinase C) family protein kinases, resulting in their activation. Previous structural studies have revealed that the alpha C-helix, located in the small lobe of the kinase domain of PDK1, is a key regulatory element, as it links a substrate interacting site termed the hydrophobic motif (HM) pocket with the phosphorylated Ser-241 in the T-loop. In this study we have demonstrated by mutational analysis that interactions between the phosphorylated Ser-241 and the alpha C-helix are not required for PDK1 activity or substrate binding through the HM-pocket but are necessary for PDK1 to be activated or stabilized by a peptide that binds to this site. The structure of an inactive T-loop mutant of PDK1, in which Ser-241 is changed to Ala, was also determined. This structure, together with surface plasmon resonance binding studies, demonstrates that the PDK1(S241A)-inactive mutant possesses an intact HM-pocket as well as an ordered alpha C-helix. These findings reveal that the integrity of the alpha C-helix and HM-pocket in PDK1 is not regulated by T-loop phosphorylation.

About this Structure

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

Reference

Role of T-loop phosphorylation in PDK1 activation, stability, and substrate binding., Komander D, Kular G, Deak M, Alessi DR, van Aalten DM, J Biol Chem. 2005 May 13;280(19):18797-802. Epub 2005 Mar 1. PMID:15741170 Page seeded by OCA on Sat May 3 20:21:20 2008

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