2biy: Difference between revisions
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==Overview== | ==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., ... | 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== | ==About this Structure== | ||
2BIY is a | 2BIY is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with SO4, ATP and GOL as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Structure known Active Site: BC6. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2BIY OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: transferase]] | [[Category: transferase]] | ||
''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 5 15:22:26 2007'' | ||
