Genetic and Pharmacological Inhibition of PDK1 in Cancer Cells: CHARACTERIZATION OF A SELECTIVE ALLOSTERIC KINASE INHIBITOR

scientific article

Genetic and Pharmacological Inhibition of PDK1 in Cancer Cells: CHARACTERIZATION OF A SELECTIVE ALLOSTERIC KINASE INHIBITOR is …
instance of (P31):
scholarly articleQ13442814

External links are
P356DOI10.1074/JBC.M110.156463
P3181OpenCitations bibliographic resource ID1914748
P932PMC publication ID3057779
P698PubMed publication ID21118801

P50authorMaciej WiznerowiczQ90207653
Alan B. NorthrupQ108812188
P2093author name stringAn Chi
Youwei Yan
Sanjeev K Munshi
Anke Klippel
Lixia Li
Manfred Kraus
Ekaterina V Bobkova
Heike Keilhack
Uwe Mueller
Sriram Sathyanarayanan
Jannik N Andersen
Alexander A Szewczak
Bart A Lutterbach
Bo-Sheng Pan
Brian Dolinski
Kumiko Nagashima
Albert H Chen
Peter Blume-Jensen
Sujal Deshmukh
Zangwei Xu
Youyuan Xu
Thi Nguyen
Stuart D Shumway
Victoria Richon
Cloud Paweletz
Roy Pollock
Timothy Allison
P2860cites workPDK1, the master regulator of AGC kinase signal transductionQ24297416
Survival of cancer cells is maintained by EGFR independent of its kinase activityQ24309274
Translocation of PDK-1 to the plasma membrane is important in allowing PDK-1 to activate protein kinase BQ24309564
P-TEN, the tumor suppressor from human chromosome 10q23, is a dual-specificity phosphataseQ24322705
The protein kinase complement of the human genomeQ24324497
3-Phosphoinositide-dependent protein kinase-1 (PDK1): structural and functional homology with the Drosophila DSTPK61 kinaseQ24336639
The PI3K-PDK1 connection: more than just a road to PKBQ24531972
A phosphoserine/threonine-binding pocket in AGC kinases and PDK1 mediates activation by hydrophobic motif phosphorylationQ24534951
PKN3 is required for malignant prostate cell growth downstream of activated PI 3-kinaseQ24563328
The selectivity of protein kinase inhibitors: a further updateQ24654622
Exploring the sequence space for tetracycline-dependent transcriptional activators: novel mutations yield expanded range and sensitivityQ24676926
Structural mechanism for STI-571 inhibition of abelson tyrosine kinaseQ27627097
Inhibition of p38 MAP kinase by utilizing a novel allosteric binding siteQ27638349
Structural basis for UCN-01 (7-hydroxystaurosporine) specificity and PDK1 (3-phosphoinositide-dependent protein kinase-1) inhibitionQ27641764
Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activityQ27644970
Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 2: optimization of BX-517Q27645157
Mutation of the PDK1 PH Domain Inhibits Protein Kinase B/Akt, Leading to Small Size and Insulin ResistanceQ27650096
Small Molecule Recognition of c-Src via the Imatinib-Binding ConformationQ27652602
Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAFQ28251989
Role of a novel PH-kinase domain interface in PKB/Akt regulation: structural mechanism for allosteric inhibitionQ28474624
Scaffolding function of PAK in the PDK1-Akt pathwayQ28570522
The evolution of phosphatidylinositol 3-kinases as regulators of growth and metabolismQ29547302
mTOR inhibition induces upstream receptor tyrosine kinase signaling and activates AktQ29547767
PI3K pathway alterations in cancer: variations on a themeQ29615530
Rational design of inhibitors that bind to inactive kinase conformationsQ29617558
Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activityQ29618117
3-phosphoinositide-dependent protein kinase-1 (PDK1) promotes invasion and activation of matrix metalloproteinasesQ33237192
UCN-01 in combination with topotecan in patients with advanced recurrent ovarian cancer: a study of the Princess Margaret Hospital Phase II consortiumQ33375423
Development of high-throughput TR-FRET and AlphaScreen assays for identification of potent inhibitors of PDK1.Q33509961
Efficient identification of novel leads by dynamic focused screening: PDK1 case studQ33538837
ErbB2, but not ErbB1, reinitiates proliferation and induces luminal repopulation in epithelial aciniQ34187916
Use of three-dimensional basement membrane cultures to model oncogene-induced changes in mammary epithelial morphogenesisQ34789986
Small-molecule inhibitors of PDK1.Q34869089
AKT-independent signaling downstream of oncogenic PIK3CA mutations in human cancerQ34990362
Signalling by PI3K isoforms: insights from gene-targeted mice.Q36092041
Building mammalian signalling pathways with RNAi screensQ36404147
Potentiation of antileukemic therapies by the dual PI3K/PDK-1 inhibitor, BAG956: effects on BCR-ABL- and mutant FLT3-expressing cellsQ36508937
Tuning silence: conditional systems for RNA interferenceQ36575390
Elevated phosphorylation and activation of PDK-1/AKT pathway in human breast cancerQ36614997
Analysis of 3-phosphoinositide-dependent kinase-1 signaling and function in ES cellsQ36865347
Drug discovery approaches targeting the PI3K/Akt pathway in cancerQ37270455
3-Phosphoinositide-dependent kinase 1 potentiates upstream lesions on the phosphatidylinositol 3-kinase pathway in breast carcinomaQ37307044
Genetic deletion of the Pten tumor suppressor gene promotes cell motility by activation of Rac1 and Cdc42 GTPasesQ38525479
Use of the pharmacological inhibitor BX795 to study the regulation and physiological roles of TBK1 and IkappaB kinase epsilon: a distinct upstream kinase mediates Ser-172 phosphorylation and activationQ39869345
OSU-03012, a novel celecoxib derivative, induces reactive oxygen species-related autophagy in hepatocellular carcinomaQ39916403
PDK1 regulates cancer cell motility by antagonising inhibition of ROCK1 by RhoE.Q40023259
Activation of PI3K-Akt signaling pathway promotes prostate cancer cell invasionQ40123342
Rapid generation of single-tumor spheroids for high-throughput cell function and toxicity analysisQ40231706
In vivo role of the phosphate groove of PDK1 defined by knockin mutationQ40362971
Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1.Q40445871
Direct comparison of the specificity of gene silencing using antisense oligonucleotides and RNAi.Q40469795
Roles of PDK-1 and PKN in regulating cell migration and cortical actin formation of PTEN-knockout cellsQ40494536
From the cyclooxygenase-2 inhibitor celecoxib to a novel class of 3-phosphoinositide-dependent protein kinase-1 inhibitorsQ40543789
GeneBlocs are powerful tools to study and delineate signal transduction processes that regulate cell growth and transformationQ40712978
Deficiency of PDK1 in liver results in glucose intolerance, impairment of insulin-regulated gene expression and liver failureQ41824865
Live-cell molecular analysis of Akt activation reveals roles for activation loop phosphorylationQ42823745
Phosphatidylinositol 3-kinase and NF-kappaB regulate motility of invasive MDA-MB-231 human breast cancer cells by the secretion of urokinase-type plasminogen activatorQ43786822
Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitorQ43948616
The survival pathways phosphatidylinositol-3 kinase (PI3-K)/phosphoinositide-dependent protein kinase 1 (PDK1)/Akt modulate liver regeneration through hepatocyte size rather than proliferation.Q46208944
Highly prevalent genetic alterations in receptor tyrosine kinases and phosphatidylinositol 3-kinase/akt and mitogen-activated protein kinase pathways in anaplastic and follicular thyroid cancersQ46585245
Allosteric inhibitors of Akt1 and Akt2: a naphthyridinone with efficacy in an A2780 tumor xenograft modelQ46595969
The structural basis of Janus kinase 2 inhibition by a potent and specific pan-Janus kinase inhibitorQ46713383
Hypomorphic mutation of PDK1 suppresses tumorigenesis in PTEN(+/-) miceQ46768791
The role of 3-phosphoinositide-dependent protein kinase 1 in activating AGC kinases defined in embryonic stem cellsQ57272881
Application of a human tumor colony-forming assay to new drug screeningQ70084884
Clonogenic assay with established human tumour xenografts: correlation of in vitro to in vivo activity as a basis for anticancer drug discoveryQ80032618
Phase I and pharmacokinetic study of 7-hydroxystaurosporine and carboplatin in advanced solid tumorsQ80249404
P4510describes a project that usesImageQuantQ112270642
P433issue8
P407language of work or nameEnglishQ1860
P921main subjectcell biologyQ7141
pharmacologyQ128406
allosteric inhibitorQ70361704
P304page(s)6433-48
P577publication date2011-02-25
P1433published inJournal of Biological ChemistryQ867727
P1476titleGenetic and Pharmacological Inhibition of PDK1 in Cancer Cells: CHARACTERIZATION OF A SELECTIVE ALLOSTERIC KINASE INHIBITOR
P478volume286

Reverse relations

cites work (P2860)
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