(Q34869089)

5 August 2017

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title

Small-molecule inhibitors of PDK1. (English)

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5 August 2017

Dario R Alessi

2

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author name string

Christian Peifer

series ordinal

1

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5 August 2017

publication date

1 December 2008

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5 August 2017

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5 August 2017

volume

3

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5 August 2017

issue

12

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5 August 2017

page(s)

1810-1838

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Structure, regulation and function of PKB/AKT--a major therapeutic target

5 August 2017

cites work

1 reference

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Microscopic modes and free energies of 3-phosphoinositide-dependent kinase-1 (PDK1) binding with celecoxib and other inhibitors.

21 January 2018

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Protein kinases--the major drug targets of the twenty-first century?

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7 January 2021

Oncogenic kinase signalling

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7 January 2021

Structural insights into the regulation of PDK1 by phosphoinositides and inositol phosphates.

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7 January 2021

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

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7 January 2021

Essential role of PDK1 in regulating cell size and development in mice

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7 January 2021

Phosphorylation and activation of p70s6k by PDK1

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7 January 2021

PDK1, the master regulator of AGC kinase signal transduction

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7 January 2021

TOR regulation of AGC kinases in yeast and mammals

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7 January 2021

Synthesis and function of 3-phosphorylated inositol lipids

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7 January 2021

PI3K-Akt pathway: its functions and alterations in human cancer

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7 January 2021

PDK1 regulates cancer cell motility by antagonising inhibition of ROCK1 by RhoE.

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7 January 2021

The role of 3-phosphoinositide-dependent protein kinase 1 in activating AGC kinases defined in embryonic stem cells

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7 January 2021

Deficiency of PDK1 in cardiac muscle results in heart failure and increased sensitivity to hypoxia

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7 January 2021

Deficiency of PDK1 in liver results in glucose intolerance, impairment of insulin-regulated gene expression and liver failure

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7 January 2021

Hypomorphic mutation of PDK1 suppresses tumorigenesis in PTEN(+/-) mice

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7 January 2021

Tenets of PTEN tumor suppression

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7 January 2021

Targeting the phosphatidylinositol 3-kinase pathway in airway smooth muscle: rationale and promise

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7 January 2021

Fragment approaches in structure-based drug discovery

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7 January 2021

Analysis of 3-phosphoinositide-dependent kinase-1 signaling and function in ES cells

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7 January 2021

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

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7 January 2021

Phosphorylation of Ser-241 is essential for the activity of 3-phosphoinositide-dependent protein kinase-1: identification of five sites of phosphorylation in vivo

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7 January 2021

A small molecule-kinase interaction map for clinical kinase inhibitors

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7 January 2021

The selectivity of protein kinase inhibitors: a further update

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7 January 2021

Design, synthesis, and biological evaluation of 3,4-diarylmaleimides as angiogenesis inhibitors

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7 January 2021

The protein kinase Cbeta-selective inhibitor, Enzastaurin (LY317615.HCl), suppresses signaling through the AKT pathway, induces apoptosis, and suppresses growth of human colon cancer and glioblastoma xenografts

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7 January 2021

Comparison of the ATP binding sites of protein kinases using conformationally diverse bisindolylmaleimides

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7 January 2021

Molecular basis for sunitinib efficacy and future clinical development

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7 January 2021

Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity

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7 January 2021

Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 2: optimization of BX-517

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7 January 2021

Application of meso scale technology for the measurement of phosphoproteins in human tumor xenografts

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7 January 2021

The PIF-binding pocket in PDK1 is essential for activation of S6K and SGK, but not PKB.

1 reference

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7 January 2021

Protein kinase B/Akt at a glance

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7 January 2021

Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1.

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7 January 2021

Toward a pharmacophore for kinase frequent hitters

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7 January 2021

Selectivity-determining residues in Plk1

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7 January 2021

Glivec (STI571, imatinib), a rationally developed, targeted anticancer drug

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7 January 2021

Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor

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7 January 2021

Synthesis and evaluation of substituted benzoisoquinolinones as potent inhibitors of Chk1 kinase

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7 January 2021

Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway

1 reference

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7 January 2021

Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity

1 reference

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7 January 2021

A new series of neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase

1 reference

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7 January 2021

From the cyclooxygenase-2 inhibitor celecoxib to a novel class of 3-phosphoinositide-dependent protein kinase-1 inhibitors

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.200800195

7 January 2021

2-amino-N-{4-[5-(2-phenanthrenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]-phenyl} acetamide (OSU-03012), a celecoxib derivative, directly targets p21-activated kinase

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7 January 2021

Crystal structure of the T315I mutant of AbI kinase

1 reference

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7 January 2021

Structure-guided design of pyrazolo[1,5-a]pyrimidines as inhibitors of human cyclin-dependent kinase 2.

1 reference

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7 January 2021

Identification of inhibitors of protein kinase B using fragment-based lead discovery

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7 January 2021

Development of pyrimidine-based inhibitors of Janus tyrosine kinase 3

1 reference

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7 January 2021

Discovery of dibenzo[c,f][2,7]naphthyridines as potent and selective 3-phosphoinositide-dependent kinase-1 inhibitors

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.200800195

7 January 2021

3-Hydroxyanthranilic acid inhibits PDK1 activation and suppresses experimental asthma by inducing T cell apoptosis

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.200800195

7 January 2021

Allosteric activation of the protein kinase PDK1 with low molecular weight compounds

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.200800195

7 January 2021

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

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.200800195

7 January 2021

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

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.200800195

7 January 2021

Identifiers

DOI

10.1002/CMDC.200800195

1 reference

5 August 2017

1 reference