Published in J Cell Mol Med on January 28, 2010
The pseudokinase domain of JAK2 is a dual-specificity protein kinase that negatively regulates cytokine signaling. Nat Struct Mol Biol (2011) 2.20
Biology and significance of the JAK/STAT signalling pathways. Growth Factors (2012) 1.29
Crystal structures of the JAK2 pseudokinase domain and the pathogenic mutant V617F. Nat Struct Mol Biol (2012) 1.25
Oncogenic JAK1 and JAK2-activating mutations resistant to ATP-competitive inhibitors. Haematologica (2011) 1.12
The Jak/STAT pathway. Cold Spring Harb Perspect Biol (2012) 1.11
Structure of a pseudokinase-domain switch that controls oncogenic activation of Jak kinases. Nat Struct Mol Biol (2013) 1.01
The use of structural biology in Janus kinase targeted drug discovery. Curr Drug Targets (2011) 0.99
The role of the Janus-faced transcription factor PAX5-JAK2 in acute lymphoblastic leukemia. Blood (2014) 0.94
Molecular basis for pseudokinase-dependent autoinhibition of JAK2 tyrosine kinase. Nat Struct Mol Biol (2014) 0.93
JAK2 mutants (e.g., JAK2V617F) and their importance as drug targets in myeloproliferative neoplasms. JAKSTAT (2013) 0.91
Transforming JAK1 mutations exhibit differential signalling, FERM domain requirements and growth responses to interferon-γ. Biochem J (2010) 0.88
JAK2 activation by growth hormone and other cytokines. Biochem J (2015) 0.85
TYK2 kinase activity is required for functional type I interferon responses in vivo. PLoS One (2012) 0.84
Analysis of Jak2 catalytic function by peptide microarrays: the role of the JH2 domain and V617F mutation. PLoS One (2011) 0.83
Cooperative effects of Janus and Aurora kinase inhibition by CEP701 in cells expressing Jak2V617F. J Cell Mol Med (2013) 0.82
The molecular basis of IL-10 function: from receptor structure to the onset of signaling. Curr Top Microbiol Immunol (2014) 0.80
STAT5 acetylation: Mechanisms and consequences for immunological control and leukemogenesis. JAKSTAT (2013) 0.80
Molecular insights into regulation of JAK2 in myeloproliferative neoplasms. Blood (2015) 0.78
The biology, pathogenesis and clinical aspects of acute lymphoblastic leukemia in children with Down syndrome. Leukemia (2016) 0.78
ATP binding to the pseudokinase domain of JAK2 is critical for pathogenic activation. Proc Natl Acad Sci U S A (2015) 0.78
Contribution of JAK2 mutations to T-cell lymphoblastic lymphoma development. Leukemia (2015) 0.77
JAK2-V617F-induced MAPK activity is regulated by PI3K and acts synergistically with PI3K on the proliferation of JAK2-V617F-positive cells. JAKSTAT (2013) 0.76
A structure-function perspective of Jak2 mutations and implications for alternate drug design strategies: the road not taken. Curr Med Chem (2011) 0.75
Mutations of the BRAF gene in human cancer. Nature (2002) 65.42
A census of human cancer genes. Nat Rev Cancer (2004) 36.20
Acquired resistance of lung adenocarcinomas to gefitinib or erlotinib is associated with a second mutation in the EGFR kinase domain. PLoS Med (2005) 25.93
WHAT IF: a molecular modeling and drug design program. J Mol Graph (1990) 24.35
A gain-of-function mutation of JAK2 in myeloproliferative disorders. N Engl J Med (2005) 21.48
Acquired mutation of the tyrosine kinase JAK2 in human myeloproliferative disorders. Lancet (2005) 18.59
A unique clonal JAK2 mutation leading to constitutive signalling causes polycythaemia vera. Nature (2005) 18.43
Activating mutation in the tyrosine kinase JAK2 in polycythemia vera, essential thrombocythemia, and myeloid metaplasia with myelofibrosis. Cancer Cell (2005) 17.41
A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol (2008) 14.74
Multiple BCR-ABL kinase domain mutations confer polyclonal resistance to the tyrosine kinase inhibitor imatinib (STI571) in chronic phase and blast crisis chronic myeloid leukemia. Cancer Cell (2002) 13.03
The conformational plasticity of protein kinases. Cell (2002) 11.21
Principles of interleukin (IL)-6-type cytokine signalling and its regulation. Biochem J (2003) 10.77
An allosteric mechanism for activation of the kinase domain of epidermal growth factor receptor. Cell (2006) 10.28
A chemical switch for inhibitor-sensitive alleles of any protein kinase. Nature (2000) 10.16
Targeting cancer with small molecule kinase inhibitors. Nat Rev Cancer (2009) 9.26
A family of cytokine-inducible inhibitors of signalling. Nature (1997) 9.22
JAK2 exon 12 mutations in polycythemia vera and idiopathic erythrocytosis. N Engl J Med (2007) 8.18
The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP. Proc Natl Acad Sci U S A (2008) 8.08
MPLW515L is a novel somatic activating mutation in myelofibrosis with myeloid metaplasia. PLoS Med (2006) 7.95
Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib. Proc Natl Acad Sci U S A (2005) 6.82
A new protein containing an SH2 domain that inhibits JAK kinases. Nature (1997) 6.28
Widespread occurrence of the JAK2 V617F mutation in chronic myeloproliferative disorders. Blood (2005) 6.05
Structure and function of a new STAT-induced STAT inhibitor. Nature (1997) 6.02
MPL515 mutations in myeloproliferative and other myeloid disorders: a study of 1182 patients. Blood (2006) 5.95
Identification of an acquired JAK2 mutation in polycythemia vera. J Biol Chem (2005) 5.58
Structural bioinformatics-based design of selective, irreversible kinase inhibitors. Science (2005) 5.53
Interleukin-10 and related cytokines and receptors. Annu Rev Immunol (2004) 5.41
Activating mutation of D835 within the activation loop of FLT3 in human hematologic malignancies. Blood (2001) 5.17
JAK mutations in high-risk childhood acute lymphoblastic leukemia. Proc Natl Acad Sci U S A (2009) 4.98
Polymorphisms in the tyrosine kinase 2 and interferon regulatory factor 5 genes are associated with systemic lupus erythematosus. Am J Hum Genet (2005) 4.80
Emerging roles of pseudokinases. Trends Cell Biol (2006) 4.48
The JAK2 inhibitor AZD1480 potently blocks Stat3 signaling and oncogenesis in solid tumors. Cancer Cell (2009) 4.47
Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition. Nat Struct Mol Biol (2004) 4.40
A TEL-JAK2 fusion protein with constitutive kinase activity in human leukemia. Science (1997) 4.29
Jaks and Stats in signaling by the cytokine receptor superfamily. Trends Genet (1995) 4.19
Surface comparison of active and inactive protein kinases identifies a conserved activation mechanism. Proc Natl Acad Sci U S A (2006) 4.09
Features of selective kinase inhibitors. Chem Biol (2005) 4.07
Structure of the ERM protein moesin reveals the FERM domain fold masked by an extended actin binding tail domain. Cell (2000) 3.94
Somatic mutations and germline sequence variants in the expressed tyrosine kinase genes of patients with de novo acute myeloid leukemia. Blood (2008) 3.89
Expression of Jak2V617F causes a polycythemia vera-like disease with associated myelofibrosis in a murine bone marrow transplant model. Blood (2006) 3.88
PI3Kgamma modulates the cardiac response to chronic pressure overload by distinct kinase-dependent and -independent effects. Cell (2004) 3.87
The unfolded protein response signals through high-order assembly of Ire1. Nature (2008) 3.87
Bypassing a kinase activity with an ATP-competitive drug. Science (2003) 3.71
Mutations of JAK2 in acute lymphoblastic leukaemias associated with Down's syndrome. Lancet (2008) 3.69
Activation of the tumour suppressor kinase LKB1 by the STE20-like pseudokinase STRAD. EMBO J (2003) 3.62
Janus kinases in immune cell signaling. Immunol Rev (2009) 3.60
Engineering unnatural nucleotide specificity for Rous sarcoma virus tyrosine kinase to uniquely label its direct substrates. Proc Natl Acad Sci U S A (1997) 3.59
Ratio of mutant JAK2-V617F to wild-type Jak2 determines the MPD phenotypes in transgenic mice. Blood (2007) 3.52
Crystal structure of the tyrosine phosphatase SHP-2. Cell (1998) 3.48
JAK2V617F expression in murine hematopoietic cells leads to MPD mimicking human PV with secondary myelofibrosis. Blood (2006) 3.37
Chemical genetic analysis of the time course of signal transduction by JNK. Mol Cell (2006) 3.32
High-throughput sequence analysis of the tyrosine kinome in acute myeloid leukemia. Blood (2008) 3.30
Somatically acquired JAK1 mutations in adult acute lymphoblastic leukemia. J Exp Med (2008) 3.24
Identification of driver and passenger mutations of FLT3 by high-throughput DNA sequence analysis and functional assessment of candidate alleles. Cancer Cell (2007) 3.23
Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor. Science (2003) 3.19
Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase. Cancer Res (2004) 3.13
Expression of a homodimeric type I cytokine receptor is required for JAK2V617F-mediated transformation. Proc Natl Acad Sci U S A (2005) 2.94
A chemical-genetic approach to studying neurotrophin signaling. Neuron (2005) 2.93
Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera. Cancer Cell (2008) 2.80
Nonleadlikeness and leadlikeness in biochemical screening. Drug Discov Today (2003) 2.78
Fusion of TEL, the ETS-variant gene 6 (ETV6), to the receptor-associated kinase JAK2 as a result of t(9;12) in a lymphoid and t(9;15;12) in a myeloid leukemia. Blood (1997) 2.75
An alternative inhibitor overcomes resistance caused by a mutation of the epidermal growth factor receptor. Cancer Res (2005) 2.72
Activating alleles of JAK3 in acute megakaryoblastic leukemia. Cancer Cell (2006) 2.69
Magic bullets for protein kinases. Trends Cell Biol (2001) 2.65
Pegylated interferon-alfa-2a induces complete hematologic and molecular responses with low toxicity in polycythemia vera. Blood (2008) 2.55
TG101209, a small molecule JAK2-selective kinase inhibitor potently inhibits myeloproliferative disorder-associated JAK2V617F and MPLW515L/K mutations. Leukemia (2007) 2.49
Structural basis of the membrane-targeting and unmasking mechanisms of the radixin FERM domain. EMBO J (2000) 2.49
A second-site suppressor strategy for chemical genetic analysis of diverse protein kinases. Nat Methods (2005) 2.47
Two novel protein-tyrosine kinases, each with a second phosphotransferase-related catalytic domain, define a new class of protein kinase. Mol Cell Biol (1991) 2.47
Structure-guided development of affinity probes for tyrosine kinases using chemical genetics. Nat Chem Biol (2007) 2.43
Molecular pathogenesis and therapy of polycythemia induced in mice by JAK2 V617F. PLoS One (2006) 2.42
Specific JAK2 mutation (JAK2R683) and multiple gene deletions in Down syndrome acute lymphoblastic leukemia. Blood (2008) 2.41
The structural basis of Janus kinase 2 inhibition by a potent and specific pan-Janus kinase inhibitor. Blood (2005) 2.41
New insight into BRAF mutations in cancer. Curr Opin Genet Dev (2007) 2.40
A semisynthetic epitope for kinase substrates. Nat Methods (2007) 2.40
Design of allele-specific inhibitors to probe protein kinase signaling. Curr Biol (1998) 2.36
Structure of the pseudokinase VRK3 reveals a degraded catalytic site, a highly conserved kinase fold, and a putative regulatory binding site. Structure (2009) 2.33
JNK2 is a positive regulator of the cJun transcription factor. Mol Cell (2006) 2.32
JAK2 inhibitor therapy in myeloproliferative disorders: rationale, preclinical studies and ongoing clinical trials. Leukemia (2007) 2.31
Identification of positive-acting domains in GCN2 protein kinase required for translational activation of GCN4 expression. Mol Cell Biol (1990) 2.26
Regulation of the Jak2 tyrosine kinase by its pseudokinase domain. Mol Cell Biol (2000) 2.25
Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor. Bioorg Med Chem Lett (2002) 2.21
Cytokines and immunodeficiency diseases: critical roles of the gamma(c)-dependent cytokines interleukins 2, 4, 7, 9, 15, and 21, and their signaling pathways. Immunol Rev (2004) 2.18
The pseudokinase domain is required for suppression of basal activity of Jak2 and Jak3 tyrosine kinases and for cytokine-inducible activation of signal transduction. J Biol Chem (2002) 2.14
The N-terminal domain of Janus kinase 2 is required for Golgi processing and cell surface expression of erythropoietin receptor. Mol Cell (2001) 2.10
Somatic mutations of JAK2 exon 12 in patients with JAK2 (V617F)-negative myeloproliferative disorders. Blood (2007) 2.10
Chemical genetics: where genetics and pharmacology meet. Cell (2007) 2.09
Therapeutic targeting of Janus kinases. Immunol Rev (2008) 2.03
Characterization of murine JAK2V617F-positive myeloproliferative disease. Cancer Res (2006) 1.97
Identification of novel FLT-3 Asp835 mutations in adult acute myeloid leukaemia. Br J Haematol (2001) 1.94
Selectivity and therapeutic inhibition of kinases: to be or not to be? Nat Immunol (2009) 1.92
Regulation of Jak2 through the ubiquitin-proteasome pathway involves phosphorylation of Jak2 on Y1007 and interaction with SOCS-1. Mol Cell Biol (2002) 1.92
Hitting the target: emerging technologies in the search for kinase substrates. Sci STKE (2002) 1.91
Somatic mutations of JAK1 and JAK3 in acute leukemias and solid cancers. Clin Cancer Res (2008) 1.90
The t(8;9)(p22;p24) is a recurrent abnormality in chronic and acute leukemia that fuses PCM1 to JAK2. Cancer Res (2005) 1.84
The frequency of JAK2 exon 12 mutations in idiopathic erythrocytosis patients with low serum erythropoietin levels. Haematologica (2007) 1.83
Development of ET, primary myelofibrosis and PV in mice expressing JAK2 V617F. Leukemia (2007) 1.81
Engineering Src family protein kinases with unnatural nucleotide specificity. Chem Biol (1998) 1.81
Principles of interleukin (IL)-6-type cytokine signalling and its regulation. Biochem J (2003) 10.77
Jak1 has a dominant role over Jak3 in signal transduction through γc-containing cytokine receptors. Chem Biol (2011) 2.05
Activation of STAT3 by IL-6 and IL-10 in primary human macrophages is differentially modulated by suppressor of cytokine signaling 3. J Immunol (2003) 1.92
Signatures of microRNAs and selected microRNA target genes in human melanoma. Cancer Res (2010) 1.90
Sustained IL-6/STAT-3 signaling in cholangiocarcinoma cells due to SOCS-3 epigenetic silencing. Gastroenterology (2006) 1.68
A cost effective non-commercial ECL-solution for Western blot detections yielding strong signals and low background. J Immunol Methods (2006) 1.50
Jaks and cytokine receptors--an intimate relationship. Biochem Pharmacol (2006) 1.50
SHP2 and SOCS3 contribute to Tyr-759-dependent attenuation of interleukin-6 signaling through gp130. J Biol Chem (2002) 1.48
Nucleocytoplasmic shuttling of persistently activated STAT3. J Cell Sci (2007) 1.31
Suppressor of cytokine signaling-3 is recruited to the activated granulocyte-colony stimulating factor receptor and modulates its signal transduction. J Immunol (2002) 1.29
Cross-regulation of cytokine signalling: pro-inflammatory cytokines restrict IL-6 signalling through receptor internalisation and degradation. J Cell Sci (2010) 1.17
Identification of the critical sequence elements in the cytoplasmic domain of leptin receptor isoforms required for Janus kinase/signal transducer and activator of transcription activation by receptor heterodimers. Mol Endocrinol (2002) 1.16
A new high affinity binding site for suppressor of cytokine signaling-3 on the erythropoietin receptor. Eur J Biochem (2002) 1.12
The Jak1 SH2 domain does not fulfill a classical SH2 function in Jak/STAT signaling but plays a structural role for receptor interaction and up-regulation of receptor surface expression. J Biol Chem (2005) 1.10
Long term association of the cytokine receptor gp130 and the Janus kinase Jak1 revealed by FRAP analysis. J Biol Chem (2003) 1.10
Promoter-hypermethylation is causing functional relevant downregulation of methylthioadenosine phosphorylase (MTAP) expression in hepatocellular carcinoma. Carcinogenesis (2005) 1.09
The matrix metalloproteinase 9 (mmp-9) hemopexin domain is a novel gelatin binding domain and acts as an antagonist. J Biol Chem (2002) 1.08
Interleukin-27 displays interferon-gamma-like functions in human hepatoma cells and hepatocytes. Hepatology (2009) 1.07
New target genes of MITF-induced microRNA-211 contribute to melanoma cell invasion. PLoS One (2013) 1.06
Akt modulates STAT3-mediated gene expression through a FKHR (FOXO1a)-dependent mechanism. J Biol Chem (2002) 1.04
Cell density dependent increase of constitutive signal transducers and activators of transcription 3 activity in melanoma cells is mediated by Janus kinases. Mol Cancer Res (2007) 1.02
Novel role of Janus kinase 1 in the regulation of oncostatin M receptor surface expression. J Biol Chem (2002) 1.01
Interferon-γ-induced activation of Signal Transducer and Activator of Transcription 1 (STAT1) up-regulates the tumor suppressing microRNA-29 family in melanoma cells. Cell Commun Signal (2012) 1.00
STAT3 is enriched in nuclear bodies. J Cell Sci (2003) 1.00
The role of the inhibitors of interleukin-6 signal transduction SHP2 and SOCS3 for desensitization of interleukin-6 signalling. Biochem J (2004) 0.98
Mechanisms of SOCS3 phosphorylation upon interleukin-6 stimulation. Contributions of Src- and receptor-tyrosine kinases. J Biol Chem (2005) 0.98
Multiple reasons for an inefficient STAT1 response upon IL-6-type cytokine stimulation. Cell Signal (2005) 0.97
Orientational constraints of the gp130 intracellular juxtamembrane domain for signaling. J Biol Chem (2002) 0.97
STAT5 contributes to interferon resistance of melanoma cells. Curr Biol (2005) 0.96
Hypoxia-inducible factor 1alpha is up-regulated by oncostatin M and participates in oncostatin M signaling. Hepatology (2009) 0.96
Dual role of the Jak1 FERM and kinase domains in cytokine receptor binding and in stimulation-dependent Jak activation. J Immunol (2008) 0.95
Are STATS arginine-methylated? J Biol Chem (2005) 0.95
Interferon-gamma-mediated growth regulation of melanoma cells: involvement of STAT1-dependent and STAT1-independent signals. J Invest Dermatol (2004) 0.95
Dynamic regulation of microRNA expression following interferon-γ-induced gene transcription. RNA Biol (2012) 0.93
JAK2 mutants (e.g., JAK2V617F) and their importance as drug targets in myeloproliferative neoplasms. JAKSTAT (2013) 0.91
Structural requirements of the interleukin-6 signal transducer gp130 for its interaction with Janus kinase 1: the receptor is crucial for kinase activation. Biochem J (2002) 0.89
STAT1 regulates p73-mediated Bax gene expression. FEBS Lett (2007) 0.88
Development of an IL-6 inhibitor based on the functional analysis of murine IL-6Ralpha(1). Chem Biol (2009) 0.87
Recombinant interleukin-24 lacks apoptosis-inducing properties in melanoma cells. PLoS One (2007) 0.87
A fusion protein of the gp130 and interleukin-6Ralpha ligand-binding domains acts as a potent interleukin-6 inhibitor. J Biol Chem (2003) 0.86
An unusual insertion in Jak2 is crucial for kinase activity and differentially affects cytokine responses. J Immunol (2009) 0.85
The chemoattractants, IL-8 and formyl-methionyl-leucyl-phenylalanine, regulate granulocyte colony-stimulating factor signaling by inducing suppressor of cytokine signaling-1 expression. J Immunol (2004) 0.85
Constitutive suppressor of cytokine signaling 3 expression confers a growth advantage to a human melanoma cell line. Mol Cancer Res (2007) 0.84
Interleukin-27 acts on hepatic stellate cells and induces signal transducer and activator of transcription 1-dependent responses. Cell Commun Signal (2010) 0.83
Cooperative effects of Janus and Aurora kinase inhibition by CEP701 in cells expressing Jak2V617F. J Cell Mol Med (2013) 0.82
Three dileucine-like motifs within the interbox1/2 region of the human oncostatin M receptor prevent efficient surface expression in the absence of an associated Janus kinase. J Biol Chem (2005) 0.82
Oncostatin M up-regulates the ER chaperone Grp78/BiP in liver cells. Biochem Pharmacol (2010) 0.81
Determinants governing the potency of STAT3 activation via the individual STAT3-recruiting motifs of gp130. Cell Signal (2005) 0.79
Bow to your partner for signaling. Nat Struct Mol Biol (2005) 0.77
Co-immunoprecipitation protocol to investigate cytokine receptor-associated proteins, e.g., Janus kinases or other associated signaling proteins. Methods Mol Biol (2013) 0.77
Signal transduction, receptors, mediators and genes: younger than ever - the 13th meeting of the Signal Transduction Society focused on aging and immunology. Cell Commun Signal (2010) 0.76
JAK2-V617F-induced MAPK activity is regulated by PI3K and acts synergistically with PI3K on the proliferation of JAK2-V617F-positive cells. JAKSTAT (2013) 0.76
Software tools of the Computis European project to process mass spectrometry images. Eur J Mass Spectrom (Chichester, Eng) (2014) 0.75