The selectivity of protein kinase inhibitors: a further update

Modulating Innate and Adaptive Immunity by (R)-Roscovitine: Potential Therapeutic Opportunity in Cystic Fibrosis

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

2000 • 4,109 citations

BAY 43-9006 Exhibits Broad Spectrum Oral Antitumor Activity and Targets the RAF/MEK/ERK Pathway and Receptor Tyrosine Kinases Involved in Tumor Progression and Angiogenesis

2004 • 3,873 citations

PD 098059 Is a Specific Inhibitor of the Activation of Mitogen-activated Protein Kinase Kinase in Vitro and in Vivo

1995 • 3,456 citations

Anorexigenic and Orexigenic Hormone Modulation of Mammalian Target of Rapamycin Complex 1 Activity and the Regulation of Hypothalamic Agouti-Related Protein mRNA Expression

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Identification of a Novel Inhibitor of Mitogen-activated Protein Kinase Kinase

1998 • 3,026 citations

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

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Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension

1997 • 2,847 citations

Regulation of Myosin Phosphatase by Rho and Rho-Associated Kinase (Rho-Kinase)

1996 • 2,843 citations

Isoquinolinesulfonamides, novel and potent inhibitors of cyclic nucleotide-dependent protein kinase and protein kinase C

1984 • 2,728 citations

SB 203580 is a specific inhibitor of a MAP kinase homologue which is stimulated by cellular stresses and interleukin‐1

1995 • 2,080 citations

Discovery of a Novel, Potent, and Src Family-selective Tyrosine Kinase Inhibitor

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Targets for Cell Cycle Arrest by the Immunosuppressant Rapamycin in Yeast

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Structural Mechanism for STI-571 Inhibition of Abelson Tyrosine Kinase

2000 • 1,770 citations

Calmodulin-dependent protein kinase kinase-β is an alternative upstream kinase for AMP-activated protein kinase

2005 • 1,518 citations

The specificities of protein kinase inhibitors: an update

2003 • 1,345 citations

Biochemical and Cellular Effects of Roscovitine, a Potent and Selective Inhibitor of the Cyclin‐Dependent Kinases cdc2, cdk2 and cdk5

1997 • 1,324 citations

A chemical switch for inhibitor-sensitive alleles of any protein kinase

2000 • 1,032 citations

Blockade of the MAP kinase pathway suppresses growth of colon tumors in vivo

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VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo

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Rottlerin, a Novel Protein Kinase Inhibitor

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Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site

2002 • 818 citations

Exploiting Chemical Libraries, Structure, and Genomics in the Search for Kinase Inhibitors

1998 • 792 citations

GSK3 inhibitors: development and therapeutic potential

2004 • 753 citations

NFAT dysregulation by increased dosage of DSCR1 and DYRK1A on chromosome 21

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An essential part for Rho–associated kinase in the transcellular invasion of tumor cells

1999 • 609 citations

A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma

2006 • 587 citations

SU6656, a Selective Src Family Kinase Inhibitor, Used To Probe Growth Factor Signaling

2000 • 577 citations

Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases

2005 • 556 citations

Activation of the Protein Kinase ERK5/BMK1 by Receptor Tyrosine Kinases

1999 • 518 citations

Structural Insights and Biological Effects of Glycogen Synthase Kinase 3-specific Inhibitor AR-A014418

2003 • 504 citations

Structural Bioinformatics-Based Design of Selective, Irreversible Kinase Inhibitors

2005 • 496 citations

MSK1 and MSK2 Are Required for the Mitogen- and Stress-Induced Phosphorylation of CREB and ATF1 in Fibroblasts

2002 • 446 citations

Wortmannin, a microbial product inhibitor of myosin light chain kinase.

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Exploring the specificity of the PI3K family inhibitor LY294002

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Discovery of a novel Raf kinase inhibitor.

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Identification and characterization of pleckstrin-homology-domain-dependent and isoenzyme-specific Akt inhibitors

2005 • 400 citations

Neurodevelopmental delay, motor abnormalities and cognitive deficits in transgenic mice overexpressing Dyrk1A (minibrain), a murine model of Down's syndrome

2001 • 382 citations

RalB GTPase-Mediated Activation of the IκB Family Kinase TBK1 Couples Innate Immune Signaling to Tumor Cell Survival

2006 • 358 citations

Roscovitine Targets, Protein Kinases and Pyridoxal Kinase

2005 • 342 citations

Exploitation of KESTREL to identify NDRG family members as physiological substrates for SGK1 and GSK3

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Pyrazole Urea-Based Inhibitors of p38 MAP Kinase: From Lead Compound to Clinical Candidate

2002 • 333 citations

An efficient proteomics method to identify the cellular targets of protein kinase inhibitors

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Regulation of the energy sensor AMP-activated protein kinase by antigen receptor and Ca2+ in T lymphocytes

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Chemical Genetic Analysis of the Time Course of Signal Transduction by JNK

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Conversion of SB 203580-insensitive MAP kinase family members to drug-sensitive forms by a single amino-acid substitution

1998 • 309 citations

Identification of Novel Inhibitors of the Transforming Growth Factor β1 (TGF-β1) Type 1 Receptor (ALK5)

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BIRB796 Inhibits All p38 MAPK Isoforms in Vitro and in Vivo

2005 • 296 citations

BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoformsin vitroandin vivo

2006 • 287 citations

Identification of the First Specific Inhibitor of p90 Ribosomal S6 Kinase (RSK) Reveals an Unexpected Role for RSK in Cancer Cell Proliferation

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Feedback control of the protein kinase TAK1 by SAPK2a/p38

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The COOH Terminus of Rho-kinase Negatively Regulates Rho-kinase Activity

1999 • 271 citations

Paradoxical activation of Raf by a novel Raf inhibitor

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Effects of MAP kinase cascade inhibitors on the MKK5/ERK5 pathway

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Design, Synthesis, and Evaluations of Substituted 3-[(3- or 4-Carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as Inhibitors of VEGF, FGF, and PDGF Receptor Tyrosine Kinases

1999 • 253 citations

Structural basis for selective inhibition of Src family kinases by PP1

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D4476, a cell‐permeant inhibitor of CK1, suppresses the site‐specific phosphorylation and nuclear exclusion of FOXO1a

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Negative Regulation of Protein Translation by Mitogen-Activated Protein Kinase-Interacting Kinases 1 and 2

2001 • 241 citations

Acquisition of Sensitivity of Stress-activated Protein Kinases to the p38 Inhibitor, SB 203580, by Alteration of One or More Amino Acids within the ATP Binding Pocket

1998 • 232 citations

Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo

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Transformation mediated by RhoA requires activity of ROCK kinases

1999 • 209 citations

Novel Small Molecule Inhibitors of 3-Phosphoinositide-dependent Kinase-1

2005 • 207 citations

Wortmannin, a Widely Used Phosphoinositide 3-Kinase Inhibitor, also Potently Inhibits Mammalian Polo-like Kinase

2005 • 201 citations

Design and Synthesis of Potent, Selective, and Orally Bioavailable Tetrasubstituted Imidazole Inhibitors of p38 Mitogen-Activated Protein Kinase

1999 • 194 citations

The Small Molecule Harmine Is an Antidiabetic Cell-Type-Specific Regulator of PPARγ Expression

2007 • 193 citations

Molecular mechanisms involved in the regulation of cytokine production by muramyl dipeptide

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Specific inhibition of cyclin-dependent kinases and cell proliferation by harmine

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[29] Assay and expression of mitogen-activated protein kinase, MAP kinase kinase, and Raf

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JNK2 Is a Positive Regulator of the cJun Transcription Factor

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Effect of SB 203580 on the activity of c-Raf in vitro and in vivo

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Rho‐kinase in human neutrophils: a role in signalling for myosin light chain phosphorylation and cell migration

1999 • 150 citations

A clickable inhibitor reveals context-dependent autoactivation of p90 RSK

2007 • 149 citations

Hypomorphic Mutation of PDK1 Suppresses Tumorigenesis in PTEN+/− Mice

2005 • 143 citations

The MAPK-activated kinase Rsk controls an acute Toll-like receptor signaling response in dendritic cells and is activated through two distinct pathways

2007 • 135 citations

Design and Synthesis of the First Generation of Novel Potent, Selective, and in Vivo Active (Benzothiazol-2-yl)acetonitrile Inhibitors of the c-Jun N-Terminal Kinase

2005 • 120 citations

Use of a drug‐resistant mutant of stress‐activated protein kinase 2a/p38 to validate the in vivo specificity of SB 203580

1999 • 115 citations

VX-680 Inhibits Aurora A and Aurora B Kinase Activity in Human Cells

2007 • 111 citations

Proteomic Characterization of the Angiogenesis Inhibitor SU6668 Reveals Multiple Impacts on Cellular Kinase Signaling

2005 • 102 citations

Intra-Arterial Infusion of Fasudil Hydrochloride for Treating Vasospasm Following Subarachnoid Haemorrhage

1999 • 96 citations

Identification of proangiogenic genes and pathways by high-throughput functional genomics: TBK1 and the IRF3 pathway

2006 • 96 citations

Characterization of a Protein Kinase B Inhibitor In Vitro and in Insulin-Treated Liver Cells

2007 • 95 citations

Role of protein kinase B and the MAP kinase cascade in mediating the EGF‐dependent inhibition of glycogen synthase kinase 3 in Swiss 3T3 cells¹

1999 • 89 citations

Synthesis of pyrazolo[3,4‐d]pyrimidine derivatives using ketene dithioacetals

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Direct synthesis of benzo[b]thiophene-2-carboxylate esters involving nitro displacement

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Protein kinase inhibitors block the stimulation of the AMP‐activated protein kinase by 5‐amino‐4‐imidazolecarboxamide riboside

2002 • 77 citations

Tpl2 (Tumor Progression Locus 2) Phosphorylation at Thr290 Is Induced by Lipopolysaccharide via an Iκ-B Kinase-β-dependent Pathway and Is Required for Tpl2 Activation by External Signals

2005 • 50 citations

Interleukin‐1 stimulated activation of the COT catalytic subunit through the phosphorylation of Thr290 and Ser62

2006 • 43 citations

Sonogashira cross-coupling reaction of 3-iodoindazoles with various terminal alkynes: a mild and flexible strategy to design 2-aza tryptamines

2002 • 40 citations

Direct inhibition of a PKA inhibitor, H-89 on KV channels in rabbit coronary arterial smooth muscle cells

2006 • 29 citations

Efficient synthesis of halohydroxypyridines by hydroxydeboronation

2004 • 26 citations

Improved Experimental Procedure for the Synthesis of the Potent MEK Inhibitor PD184352

2005 • 8 citations

414A Pharmacological properties and in vitro and in vivo antitumour activity of the potent and selective PI3 kinase inhibitor PI103

2004 • 6 citations