1h1w
From Proteopedia
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|PDB= 1h1w |SIZE=350|CAPTION= <scene name='initialview01'>1h1w</scene>, resolution 2.00Å | |PDB= 1h1w |SIZE=350|CAPTION= <scene name='initialview01'>1h1w</scene>, resolution 2.00Å | ||
|SITE= <scene name='pdbsite=PIF:Atp+Binding+Site+For+Chain+A'>PIF</scene> | |SITE= <scene name='pdbsite=PIF:Atp+Binding+Site+For+Chain+A'>PIF</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=SEP:PHOSPHOSERINE'>SEP</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=1h1w FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1h1w OCA], [http://www.ebi.ac.uk/pdbsum/1h1w PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1h1w RCSB]</span> | ||
}} | }} | ||
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High resolution crystal structure of the human PDK1 catalytic domain defines the regulatory phosphopeptide docking site., Biondi RM, Komander D, Thomas CC, Lizcano JM, Deak M, Alessi DR, van Aalten DM, EMBO J. 2002 Aug 15;21(16):4219-28. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/12169624 12169624] | High resolution crystal structure of the human PDK1 catalytic domain defines the regulatory phosphopeptide docking site., Biondi RM, Komander D, Thomas CC, Lizcano JM, Deak M, Alessi DR, van Aalten DM, EMBO J. 2002 Aug 15;21(16):4219-28. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/12169624 12169624] | ||
[[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: Lizcano, J M.]] | [[Category: Lizcano, J M.]] | ||
[[Category: Thomas, C C.]] | [[Category: Thomas, C C.]] | ||
| - | [[Category: ATP]] | ||
| - | [[Category: GOL]] | ||
| - | [[Category: SO4]] | ||
[[Category: agc kinase activation]] | [[Category: agc kinase activation]] | ||
[[Category: atp-binding]] | [[Category: atp-binding]] | ||
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[[Category: transferase]] | [[Category: transferase]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 20:55:58 2008'' |
Revision as of 17:56, 30 March 2008
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| , resolution 2.00Å | |||||||
|---|---|---|---|---|---|---|---|
| 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 | ||||||
HIGH RESOLUTION CRYSTAL STRUCTURE OF THE HUMAN PDK1 CATALYTIC DOMAIN
Overview
3-phosphoinositide dependent protein kinase-1 (PDK1) plays a key role in regulating signalling pathways by activating AGC kinases such as PKB/Akt and S6K. Here we describe the 2.0 A crystal structure of the PDK1 kinase domain in complex with ATP. The structure defines the hydrophobic pocket termed the "PIF-pocket", which plays a key role in mediating the interaction and phosphorylation of certain substrates such as S6K1. Phosphorylation of S6K1 at its C-terminal PIF-pocket-interacting motif promotes the binding of S6K1 with PDK1. In the PDK1 structure, this pocket is occupied by a crystallographic contact with another molecule of PDK1. Interestingly, close to the PIF-pocket in PDK1, there is an ordered sulfate ion, interacting tightly with four surrounding side chains. The roles of these residues were investigated through a combination of site-directed mutagenesis and kinetic studies, the results of which confirm that this region of PDK1 represents a phosphate-dependent docking site. We discuss the possibility that an analogous phosphate-binding regulatory motif may participate in the activation of other AGC kinases. Furthermore, the structure of PDK1 provides a scaffold for the design of specific PDK1 inhibitors.
About this Structure
1H1W is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
High resolution crystal structure of the human PDK1 catalytic domain defines the regulatory phosphopeptide docking site., Biondi RM, Komander D, Thomas CC, Lizcano JM, Deak M, Alessi DR, van Aalten DM, EMBO J. 2002 Aug 15;21(16):4219-28. PMID:12169624
Page seeded by OCA on Sun Mar 30 20:55:58 2008
Categories: Homo sapiens | Non-specific serine/threonine protein kinase | Single protein | Aalten, D M.F Van. | Alessi, D R. | Biondi, R M. | Deak, M. | Komander, D. | Lizcano, J M. | Thomas, C C. | Agc kinase activation | Atp-binding | Phosphoinositide dependent protein kinase | Pi3-kinase signalling | Pif-pocket | Pka | Serine/threonine-protein kinase | Transferase
