2biy
From Proteopedia
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|PDB= 2biy |SIZE=350|CAPTION= <scene name='initialview01'>2biy</scene>, resolution 1.95Å | |PDB= 2biy |SIZE=350|CAPTION= <scene name='initialview01'>2biy</scene>, resolution 1.95Å | ||
|SITE= <scene name='pdbsite=BC6:Atp+Binding+Site+For+Chain+A'>BC6</scene> | |SITE= <scene name='pdbsite=BC6:Atp+Binding+Site+For+Chain+A'>BC6</scene> | ||
| - | |LIGAND= <scene name='pdbligand= | + | |LIGAND= <scene name='pdbligand=ATP:ADENOSINE-5'-TRIPHOSPHATE'>ATP</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene> |
| - | |ACTIVITY= [http://en.wikipedia.org/wiki/ | + | |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= | ||
| + | |RELATEDENTRY= | ||
| + | |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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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:[http://www.ncbi.nlm.nih.gov/pubmed/15741170 15741170] | 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:[http://www.ncbi.nlm.nih.gov/pubmed/15741170 15741170] | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
| + | [[Category: Non-specific serine/threonine protein kinase]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| - | [[Category: Transferred entry: 2 7.11 1]] | ||
[[Category: Aalten, D M.F Van.]] | [[Category: Aalten, D M.F Van.]] | ||
[[Category: Alessi, D R.]] | [[Category: Alessi, D R.]] | ||
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[[Category: Komander, D.]] | [[Category: Komander, D.]] | ||
[[Category: Kular, G S.]] | [[Category: Kular, G S.]] | ||
| - | [[Category: ATP]] | ||
| - | [[Category: GOL]] | ||
| - | [[Category: SO4]] | ||
[[Category: ac-helix]] | [[Category: ac-helix]] | ||
[[Category: agc kinase]] | [[Category: agc kinase]] | ||
| Line 44: | Line 44: | ||
[[Category: transferase]] | [[Category: transferase]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 02:07:08 2008'' |
Revision as of 23:07, 30 March 2008
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| , resolution 1.95Å | |||||||
|---|---|---|---|---|---|---|---|
| Sites: | |||||||
| Ligands: | , , | ||||||
| Activity: | Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 | ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
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 Mon Mar 31 02:07:08 2008
Categories: Homo sapiens | Non-specific serine/threonine protein kinase | Single protein | Aalten, D M.F Van. | Alessi, D R. | Deak, M. | Komander, D. | Kular, G S. | Ac-helix | Agc kinase | Atp-binding | Phosphoinositide dependent protein kinase | Phosphorylation | Pi3-kinase signalling | Pif-pocket | Pka | Pkb | Serine-threonine-protein kinase | T-loop mutant | Transferase
