Phosphoinositide-dependent kinase 1 (PDK1) is the master regulator of at least 23 other AGC kinases whose downstream signalling has often been implicated in various diseases and in particular in cancer. Therefore there has been great interest in determining how PDK1 is controlled and how it regulates its substrates spatially and temporally. The understanding of these mechanisms could offer new possibilities for therapeutic intervention. Over the years, a more comprehensive view of the mechanisms involved in the regulation of PDK1 has emerged and these comprise serine/threonine as well as tyrosine phosphorylation, subcellular localization, regulator binding and conformation status. In the present review, we discuss how various molecular mechanisms are together responsible for the conformational regulation behind the activation of PDK1 in cells.
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October 2014
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Conference Article|
September 18 2014
Acute regulation of PDK1 by a complex interplay of molecular switches
Veronique Calleja;
Veronique Calleja
1
*Cell Biophysics Laboratory, Cancer Research UK London Research Institute, 44 Lincoln's Inn Fields, London WC2A 3LY, U.K.
†Protein Phosphorylation Laboratory, Cancer Research UK London Research Institute, 44 Lincoln's Inn Fields, London WC2A 3LY, U.K.
1To whom correspondence should be addressed at the present address: Protein Phosphorylation Laboratory, Cancer Research UK London Research Institute, 44 Lincoln's Inn Fields, London WC2A 3LY, U.K. (emailveronique.calleja@cancer.org.uk).
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Michel Laguerre;
Michel Laguerre
‡Institut Européen de Chimie et Biologie, Université de Bordeaux, UMR 5248, 2 rue Robert Escarpit, F-33607 Pessac, France
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Gloria de las Heras-Martinez;
Gloria de las Heras-Martinez
§Biophotonics Lab, Unidad de Biofísica CSIC-UPV/EHU, Barrio de Sarriena s/n, 48940 Leioa, Spain
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Peter J. Parker;
Peter J. Parker
†Protein Phosphorylation Laboratory, Cancer Research UK London Research Institute, 44 Lincoln's Inn Fields, London WC2A 3LY, U.K.
∥Division of Cancer Studies, King's College London, Guy's Campus, London SE1 1UL, U.K.
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Jose Requejo-Isidro;
Jose Requejo-Isidro
§Biophotonics Lab, Unidad de Biofísica CSIC-UPV/EHU, Barrio de Sarriena s/n, 48940 Leioa, Spain
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Banafshé Larijani
Banafshé Larijani
*Cell Biophysics Laboratory, Cancer Research UK London Research Institute, 44 Lincoln's Inn Fields, London WC2A 3LY, U.K.
¶Cell Biophysics Laboratory, Ikerbasque, Basque Foundation for Science, Plaza Bizkaia, 48011 Bilbao, Spain
**Unidad de Biofísica CSIC-UPV/EHU, Barrio de Sarriena s/n, 48940 Leioa, Spain
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Publisher: Portland Press Ltd
Received:
August 11 2014
Online ISSN: 1470-8752
Print ISSN: 0300-5127
© The Authors Journal compilation © 2014 Biochemical Society
2014
Biochem Soc Trans (2014) 42 (5): 1435–1440.
Article history
Received:
August 11 2014
Citation
Veronique Calleja, Michel Laguerre, Gloria de las Heras-Martinez, Peter J. Parker, Jose Requejo-Isidro, Banafshé Larijani; Acute regulation of PDK1 by a complex interplay of molecular switches. Biochem Soc Trans 1 October 2014; 42 (5): 1435–1440. doi: https://doi.org/10.1042/BST20140222
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