Structural basis for UCN-01 (7-hydroxystaurosporine) specificity and PDK1 (3-phosphoinositide-dependent protein kinase-1) inhibition (Q27641764)

5

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author name string

Gursant S Kular

2

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Jennifer Bain

3

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Matthew Elliott

4

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Daan M F Van Aalten

Crystal structure of an activated Akt/protein kinase B ternary complex with GSK3-peptide and AMP-PNP

6

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language of work or name

English

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publication date

15 October 2003

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published in

Biochemical Journal

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volume

375

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issue

Pt 2

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page(s)

255-62

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cites work

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Structural basis for Chk1 inhibition by UCN-01

20 March 2017

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High resolution crystal structure of the human PDK1 catalytic domain defines the regulatory phosphopeptide docking site

20 March 2017

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Structure of GSK3beta reveals a primed phosphorylation mechanism

20 March 2017

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The replacement of ATP by the competitive inhibitor emodin induces conformational modifications in the catalytic site of protein kinase CK2

20 March 2017

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Identification of a pocket in the PDK1 kinase domain that interacts with PIF and the C-terminal residues of PKA

20 March 2017

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The PI3K-PDK1 connection: more than just a road to PKB

20 March 2017

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The structure of phosphorylated p38gamma is monomeric and reveals a conserved activation-loop conformation

20 March 2017

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Structural analysis of the lymphocyte-specific kinase Lck in complex with non-selective and Src family selective kinase inhibitors

20 March 2017

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Role of phosphatidylinositol 3,4,5-trisphosphate in regulating the activity and localization of 3-phosphoinositide-dependent protein kinase-1

20 March 2017

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Structure of the protein tyrosine kinase domain of C-terminal Src kinase (CSK) in complex with staurosporine

20 March 2017

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Phosphorylation and activation of p70s6k by PDK1

20 March 2017

1 reference

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Staurosporine-induced conformational changes of cAMP-dependent protein kinase catalytic subunit explain inhibitory potential

20 March 2017

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3-Phosphoinositide-dependent protein kinase-1 (PDK1): structural and functional homology with the Drosophila DSTPK61 kinase

20 March 2017

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Protein kinase inhibition by staurosporine revealed in details of the molecular interaction with CDK2

20 March 2017

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The structure of mitogen-activated protein kinase p38 at 2.1-A resolution

20 March 2017

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Atomic structure of the MAP kinase ERK2 at 2.3 A resolution

20 March 2017

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Two structures of the catalytic domain of phosphorylase kinase: an active protein kinase complexed with substrate analogue and product

20 March 2017

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Crystal Structure of the Catalytic Subunit of Cyclic Adenosine Monophosphate-Dependent Protein Kinase

20 March 2017

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Detection, delineation, measurement and display of cavities in macromolecular structures

20 March 2017

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T-Coffee: A novel method for fast and accurate multiple sequence alignment

20 March 2017

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Crystallography & NMR System: A New Software Suite for Macromolecular Structure Determination

20 March 2017

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WHAT IF: a molecular modeling and drug design program

20 March 2017

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Improved methods for building protein models in electron density maps and the location of errors in these models

20 March 2017

1 reference

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The Chk1 protein kinase and the Cdc25C regulatory pathways are targets of the anticancer agent UCN-01

20 March 2017

1 reference

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Specificity and mechanism of action of some commonly used protein kinase inhibitors

20 March 2017

1 reference

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Casein kinase I gamma subfamily. Molecular cloning, expression, and characterization of three mammalian isoforms and complementation of defects in the Saccharomyces cerevisiae YCK genes

20 March 2017

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The protein kinase resource

20 March 2017

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The specificities of protein kinase inhibitors: an update

9 May 2017

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Signalling specificity of Ser/Thr protein kinases through docking-site-mediated interactions

9 May 2017

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The cell cycle as a target for cancer therapy: basic and clinical findings with the small molecule inhibitors flavopiridol and UCN-01.

29 September 2017

1 reference

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PTEN: The down side of PI 3-kinase signalling.

29 September 2017

1 reference

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Dynamics of cAMP-dependent protein kinase

29 September 2017

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Ten years of protein kinase B signalling: a hard Akt to follow

29 September 2017

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PKB/AKT: functional insights from genetic models

29 September 2017

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Staurosporine analogues - pharmacological toys or useful antitumour agents?

29 September 2017

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Role and regulation of 90 kDa ribosomal S6 kinase (RSK) in signal transduction.

29 September 2017

1 reference

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The packing density in proteins: standard radii and volumes.

29 September 2017

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Positioning hydrogen atoms by optimizing hydrogen-bond networks in protein structures

29 September 2017

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Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases

29 September 2017

1 reference

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UCN-01, a selective inhibitor of protein kinase C from Streptomyces.

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=1223700

Interference with PDK1-Akt survival signaling pathway by UCN-01 (7-hydroxystaurosporine).

2 June 2018

1 reference

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Discovery of PDK1, one of the missing links in insulin signal transduction. Colworth Medal Lecture.

27 November 2018

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PRODRG, a program for generating molecular topologies and unique molecular descriptors from coordinates of small molecules.

27 November 2018

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Protein kinase C inhibitors induce apoptosis in human malignant glioma cell lines

27 November 2018

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UCN-01 and UCN-02, new selective inhibitors of protein kinase C. II. Purification, physico-chemical properties, structural determination and biological activities

27 November 2018

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PubMed

https://pubmed.ncbi.nlm.nih.gov/12892559