1o6l
From Proteopedia
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| - | [[Image:1o6l.gif|left|200px]] | + | [[Image:1o6l.gif|left|200px]] |
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| - | '''CRYSTAL STRUCTURE OF AN ACTIVATED AKT/PROTEIN KINASE B (PKB-PIF CHIMERA) TERNARY COMPLEX WITH AMP-PNP AND GSK3 PEPTIDE''' | + | {{Structure |
| + | |PDB= 1o6l |SIZE=350|CAPTION= <scene name='initialview01'>1o6l</scene>, resolution 1.60Å | ||
| + | |SITE= <scene name='pdbsite=AC1:Mn+Binding+Site+For+Chain+A'>AC1</scene> | ||
| + | |LIGAND= <scene name='pdbligand=MN:MANGANESE+(II)+ION'>MN</scene> and <scene name='pdbligand=ANP:PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER'>ANP</scene> | ||
| + | |ACTIVITY= [http://en.wikipedia.org/wiki/Transferred_entry:_2.7.11.1 Transferred entry: 2.7.11.1], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.37 2.7.1.37] | ||
| + | |GENE= | ||
| + | }} | ||
| + | |||
| + | '''CRYSTAL STRUCTURE OF AN ACTIVATED AKT/PROTEIN KINASE B (PKB-PIF CHIMERA) TERNARY COMPLEX WITH AMP-PNP AND GSK3 PEPTIDE''' | ||
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==Overview== | ==Overview== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1O6L is a [ | + | 1O6L is a [[Protein complex]] structure of sequences 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=1O6L OCA]. |
==Reference== | ==Reference== | ||
| - | Crystal structure of an activated Akt/protein kinase B ternary complex with GSK3-peptide and AMP-PNP., Yang J, Cron P, Good VM, Thompson V, Hemmings BA, Barford D, Nat Struct Biol. 2002 Dec;9(12):940-4. PMID:[http:// | + | Crystal structure of an activated Akt/protein kinase B ternary complex with GSK3-peptide and AMP-PNP., Yang J, Cron P, Good VM, Thompson V, Hemmings BA, Barford D, Nat Struct Biol. 2002 Dec;9(12):940-4. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/12434148 12434148] |
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
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[[Category: transferase]] | [[Category: transferase]] | ||
| - | ''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 13:06:26 2008'' |
Revision as of 11:06, 20 March 2008
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| , resolution 1.60Å | |||||||
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| Sites: | |||||||
| Ligands: | and | ||||||
| Activity: | Transferred entry: 2.7.11.1, with EC number 2.7.1.37 | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
CRYSTAL STRUCTURE OF AN ACTIVATED AKT/PROTEIN KINASE B (PKB-PIF CHIMERA) TERNARY COMPLEX WITH AMP-PNP AND GSK3 PEPTIDE
Overview
The protein kinase Akt/PKB is stimulated by the phosphorylation of two regulatory residues, Thr 309 of the activation segment and Ser 474 of the hydrophobic motif (HM), that are structurally and functionally conserved within the AGC kinase family. To understand the mechanism of PKB regulation, we determined the crystal structures of activated kinase domains of PKB in complex with a GSK3beta-peptide substrate and an ATP analog. The activated state of the kinase was generated by phosphorylating Thr 309 using PDK1 and mimicking Ser 474 phosphorylation either with the S474D substitution or by replacing the HM of PKB with that of PIFtide, a potent mimic of a phosphorylated HM. Comparison with the inactive PKB structure indicates that the role of Ser 474 phosphorylation is to promote the engagement of the HM with the N-lobe of the kinase domain, promoting a disorder-to-order transition of the alphaC helix. The alphaC helix, by interacting with pThr 309, restructures and orders the activation segment, generating an active kinase conformation. Analysis of the interactions between PKB and the GSK3beta-peptide explains how PKB selects for protein substrates distinct from those of PKA.
About this Structure
1O6L is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.
Reference
Crystal structure of an activated Akt/protein kinase B ternary complex with GSK3-peptide and AMP-PNP., Yang J, Cron P, Good VM, Thompson V, Hemmings BA, Barford D, Nat Struct Biol. 2002 Dec;9(12):940-4. PMID:12434148
Page seeded by OCA on Thu Mar 20 13:06:26 2008
