2biy
From Proteopedia
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[[Image:2biy.gif|left|200px]] | [[Image:2biy.gif|left|200px]] | ||
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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.]] | ||
- | [[Category: | + | [[Category: Ac-helix]] |
- | [[Category: | + | [[Category: Agc kinase]] |
- | [[Category: | + | [[Category: Atp-binding]] |
- | [[Category: | + | [[Category: Phosphoinositide dependent protein kinase]] |
- | [[Category: | + | [[Category: Phosphorylation]] |
- | [[Category: | + | [[Category: Pi3-kinase signalling]] |
- | [[Category: | + | [[Category: Pif-pocket]] |
- | [[Category: | + | [[Category: Pka]] |
- | [[Category: | + | [[Category: Pkb]] |
- | [[Category: | + | [[Category: Serine-threonine-protein kinase]] |
- | [[Category: | + | [[Category: T-loop mutant]] |
- | [[Category: | + | [[Category: Transferase]] |
- | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 20:21:20 2008'' | |
- | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + |
Revision as of 17:21, 3 May 2008
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
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