Sensitivity and resistance of JAK2 inhibitors to myeloproliferative neoplasms

Intrinsic Resistance to JAK2 Inhibition in Myelofibrosis

(2013) A. Kalota et al.   CLINICAL CANCER RESEARCH

Effect of Ruxolitinib Therapy on Myelofibrosis-Related Symptoms and Other Patient-Reported Outcomes in COMFORT-I: A Randomized, Double-Blind, Placebo-Controlled Trial

(2013) Ruben A. Mesa et al.   JOURNAL OF CLINICAL ONCOLOGY

Dual PI3K/AKT/mTOR Inhibitor BEZ235 Synergistically Enhances the Activity of JAK2 Inhibitor against Cultured and Primary Human Myeloproliferative Neoplasm Cells

(2013) W. Fiskus et al.   MOLECULAR CANCER THERAPEUTICS

Long-term outcomes of 107 patients with myelofibrosis receiving JAK1/JAK2 inhibitor ruxolitinib: survival advantage in comparison to matched historical controls

(2012) S. Verstovsek et al.   BLOOD

Genetic and Pharmacologic Inhibition of β-Catenin Targets Imatinib-Resistant Leukemia Stem Cells in CML

(2012) Florian H. Heidel et al.   Cell Stem Cell

Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition

(2012) Oliver Weigert et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Heterodimeric JAK–STAT activation as a mechanism of persistence to JAK2 inhibitor therapy

(2012) Priya Koppikar et al.   NATURE

A Double-Blind, Placebo-Controlled Trial of Ruxolitinib for Myelofibrosis

(2012) Srdan Verstovsek et al.   NEW ENGLAND JOURNAL OF MEDICINE

Random Mutagenesis Reveals Residues of JAK2 Critical in Evading Inhibition by a Tyrosine Kinase Inhibitor

(2012) Michael R. Marit et al.   PLoS One

Modulation of Activation-Loop Phosphorylation by JAK Inhibitors Is Binding Mode Dependent

(2012) Rita Andraos et al.   Cancer Discovery

Safety and efficacy of everolimus, a mTOR inhibitor, as single agent in a phase 1/2 study in patients with myelofibrosis

(2011) P. Guglielmelli et al.   BLOOD

Heat Shock Protein 90 Inhibitor Is Synergistic with JAK2 Inhibitor and Overcomes Resistance to JAK2-TKI in Human Myeloproliferative Neoplasm Cells

(2011) W. Fiskus et al.   CLINICAL CANCER RESEARCH

Self-renewal related signaling in myeloid leukemia stem cells

(2011) Florian H. Heidel et al.   INTERNATIONAL JOURNAL OF HEMATOLOGY

Safety and Efficacy of TG101348, a Selective JAK2 Inhibitor, in Myelofibrosis

(2011) Animesh Pardanani et al.   JOURNAL OF CLINICAL ONCOLOGY

Characterization of BMS-911543, a functionally selective small-molecule inhibitor of JAK2

(2011) A V Purandare et al.   LEUKEMIA

Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms

(2011) A Deshpande et al.   LEUKEMIA

SB1518, a novel macrocyclic pyrimidine-based JAK2 inhibitor for the treatment of myeloid and lymphoid malignancies

(2011) S Hart et al.   LEUKEMIA

The pseudokinase domain of JAK2 is a dual-specificity protein kinase that negatively regulates cytokine signaling

(2011) Daniela Ungureanu et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Efficacy of NS-018, a potent and selective JAK2/Src inhibitor, in primary cells and mouse models of myeloproliferative neoplasms

(2011) Y Nakaya et al.   Blood Cancer Journal

Efficacy of the JAK2 inhibitor INCB16562 in a murine model of MPLW515L-induced thrombocytosis and myelofibrosis

(2010) P. Koppikar et al.   BLOOD

Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms

(2010) A. Quintas-Cardama et al.   BLOOD

Physiological Jak2V617F Expression Causes a Lethal Myeloproliferative Neoplasm with Differential Effects on Hematopoietic Stem and Progenitor Cells

(2010) Ann Mullally et al.   CANCER CELL

HSP90 is a therapeutic target in JAK2-dependent myeloproliferative neoplasms in mice and humans

(2010) Sachie Marubayashi et al.   JOURNAL OF CLINICAL INVESTIGATION

JAK inhibitor therapy for myelofibrosis: critical assessment of value and limitations

(2010) A Pardanani et al.   LEUKEMIA

Safety and Efficacy of INCB018424, a JAK1 and JAK2 Inhibitor, in Myelofibrosis

(2010) Srdan Verstovsek et al.   NEW ENGLAND JOURNAL OF MEDICINE

Phase 2 study of CEP-701, an orally available JAK2 inhibitor, in patients with primary or post-polycythemia vera/essential thrombocythemia myelofibrosis

(2009) F. P. S. Santos et al.   BLOOD

Cotreatment with panobinostat and JAK2 inhibitor TG101209 attenuates JAK2V617F levels and signaling and exerts synergistic cytotoxic effects against human myeloproliferative neoplastic cells

(2009) Y. Wang et al.   BLOOD

The JAK2 Inhibitor AZD1480 Potently Blocks Stat3 Signaling and Oncogenesis in Solid Tumors

(2009) Michael Hedvat et al.   CANCER CELL

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

(2009) A Pardanani et al.   LEUKEMIA

JAK2 phosphorylates histone H3Y41 and excludes HP1α from chromatin

(2009) Mark A. Dawson et al.   NATURE

Hedgehog signalling is essential for maintenance of cancer stem cells in myeloid leukaemia

(2009) Chen Zhao et al.   NATURE

A dynamic prognostic model to predict survival in post-polycythemia vera myelofibrosis

(2008) F. Passamonti et al.   BLOOD

Expansion of Bcr-Abl-Positive Leukemic Stem Cells Is Dependent on Hedgehog Pathway Activation

(2008) Christine Dierks et al.   CANCER CELL

Efficacy of TG101348, a Selective JAK2 Inhibitor, in Treatment of a Murine Model of JAK2V617F-Induced Polycythemia Vera

(2008) Gerlinde Wernig et al.   CANCER CELL