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Pyridone 6, A Pan-Janus-Activated Kinase Inhibitor, Suppresses Osteoclast Formation and Bone Resorption through Down-Regulation of Receptor Activator of Nuclear Factor-kappa B (NF-kappa B) Ligand (RANKL)-Induced c-Fos and Nuclear Factor of Activated T Cells (NFAT) c1 Expression
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2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2
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Discovery of pyrazol-3-ylamino pyrazines as novel JAK2 inhibitors
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2009)
Fragment-based discovery of JAK-2 inhibitors
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2009)
Identification of a novel inhibitor of JAK2 tyrosine kinase by structure-based virtual screening
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2009)
Novel strategies for patients with chronic myeloproliferative disorders
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CURRENT OPINION IN HEMATOLOGY (2009)
Prospect of JAK2 inhibitor therapy in myeloproliferative neoplasms
Ehab Atallah et al.
EXPERT REVIEW OF ANTICANCER THERAPY (2009)
Janus Kinase 2 Inhibitors. Synthesis and Characterization of a Novel Polycyclic Azaindole
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JOURNAL OF MEDICINAL CHEMISTRY (2009)
CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients
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Kinase drug discovery approaches in chronic myeloproliferative disorders
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Jak2 Inhibitors: Rationale and Role as Therapeutic Agents in Hematologic Malignancies
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JAK2 Inhibitors: A Reality? A Hope?
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CLINICAL LYMPHOMA & MYELOMA (2009)
Selective inhibition of JAK2-Driven erythroid differentiation of polycythemia vera progenitors
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CANCER CELL (2008)
Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera
Gerlinde Werning et al.
CANCER CELL (2008)
WP1066, a novel JAK2 inhibitor, suppresses proliferation and induces apoptosis in erythroid human cells carrying the JAK2 V617F mutation
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Therapeutic targeting of Janus kinases
Marko Pesu et al.
IMMUNOLOGICAL REVIEWS (2008)
Effects of the JAK2 Inhibitor, AZ960, on Pim/BAD/BCL-xL Survival Signaling in the Human JAK2 V617F Cell Line SET-2
Joseph M. Gozgit et al.
JOURNAL OF BIOLOGICAL CHEMISTRY (2008)
LS104, a non-ATP-competitive small-molecule inhibitor of JAK2, is potently inducing apoptosis in JAK2V617F-positive cells
Daniel B. Lipka et al.
MOLECULAR CANCER THERAPEUTICS (2008)
Z3, a novel Jak2 tyrosine kinase small-molecule inhibitor that suppresses Jak2-mediated pathologic cell growth
Jacqueline Sayyah et al.
MOLECULAR CANCER THERAPEUTICS (2008)
The JAK kinases: Not just another kinase drug discovery target
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Lestaurtinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disorders
Elizabeth O. Hexner et al.
BLOOD (2008)
JAK2 inhibitor therapy in myeloproliferative disorders: rationale, preclinical studies and ongoing clinical trials
A. Pardanani
LEUKEMIA (2008)
WP1066 disrupts janus kinase-2 and induces caspase-dependent apoptosis in acute myelogenous leukemia cells
Alessandra Ferrajoli et al.
CANCER RESEARCH (2007)
8-benzyl-4-oxo-8-azabicyclo[3.2.1]oct-2-ene-6,7-dicarboxylic acid (SD-1008), a novel janus kinase 2 inhibitor, increases chemotherapy sensitivity in human ovarian cancer cells
Zhenfeng Duan et al.
MOLECULAR PHARMACOLOGY (2007)
TG101209, a small molecule JAK2-selective kinase inhibitor potently inhibits myeloproliferative disorder-associated JAK2V617F and MPLW515L/K mutations
A. Pardanani et al.
LEUKEMIA (2007)
Emodin has a cytotoxic activity against human multiple myeloma as a Janus-activated kinase 2 inhibitor
Akihiro Muto et al.
MOLECULAR CANCER THERAPEUTICS (2007)
Pyridone 6, a pan-janus-activated kinase inhibitor, induces growth inhibition of multiple myeloma cells
Laura Pedranzini et al.
CANCER RESEARCH (2006)
X-inactivation-based clonality analysis and quantitative JAK2V617F assessment reveal a strong association between clonality and JAK2V617F in PV but not ET/MMM, and identifies a subset of JAK2V617F-negative ET and NIMM patients with clonal hematopoiesis
Ross L. Levine et al.
BLOOD (2006)
The structural basis of Janus kinase 2 inhibition by a potent and specific pan-Janus kinase inhibitor
IS Lucet et al.
BLOOD (2006)
A gain-of-function mutation of JAK2 in myeloproliferative disorders
R Kralovics et al.
NEW ENGLAND JOURNAL OF MEDICINE (2005)
Identification of 1,2,3,4,5,6-hexabromocyclohexane as a small molecule inhibitor of Jak2 tyrosine kinase autophophorylation
EM Sandberg et al.
JOURNAL OF MEDICINAL CHEMISTRY (2005)
Inhibitors of JAKs/STATs and the kinases: a possible new cluster of drugs
C Luo et al.
DRUG DISCOVERY TODAY (2004)
VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo
EA Harrington et al.
NATURE MEDICINE (2004)
Multiple signaling pathways are involved in erythropoietin-independent differentiation of erythroid progenitors in polycythemia vera
V Ugo et al.
EXPERIMENTAL HEMATOLOGY (2004)
Characterization of a peptide inhibitor of janus kinase 2 that mimics suppressor of cytokine signaling 1 function
LO Flowers et al.
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Granulocyte-macrophage colony-stimulating factor (GM-CSF) induces antiapoptotic and proapoptotic signals in acute myeloid leukemia
S Faderl et al.
BLOOD (2003)
Photochemical preparation of a pyridone containing tetracycle: A Jak protein kinase inhibitor
JE Thompson et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2002)
A FLT3 tyrosine kinase inhibitor is selectively cytotoxic to acute myeloid leukemia blasts harboring FLT3 internal tandem duplication mutations
M Levis et al.
BLOOD (2001)