CHZ868, a Type II JAK2 Inhibitor, Reverses Type I JAK Inhibitor Persistence and Demonstrates Efficacy in Myeloproliferative Neoplasms. (Q34485103)

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19 February 2020

title

CHZ868, a Type II JAK2 Inhibitor, Reverses Type I JAK Inhibitor Persistence and Demonstrates Efficacy in Myeloproliferative Neoplasms (English)

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19 February 2020

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ChEBI release 2020-05-28

1

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Franck Rapaport

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Ke Xu

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author name string

Matthew D Keller

2

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Sophia Chiu

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Priya Koppikar

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Olga A Guryanova

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Katia Manova

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Dmitry Pankov

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Richard J O'Reilly

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Maria Kleppe

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Anna Sophia McKenney

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Alan H Shih

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Kaitlyn Shank

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Jihae Ahn

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Eftymia Papalexi

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Barbara Spitzer

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Nick Socci

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Agnes Viale

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Emeline Mandon

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Rita Andraos

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Rona Singer Weinberg

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Ronald Hoffman

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publication date

1 July 2015

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19 February 2020

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19 February 2020

volume

28

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19 February 2020

issue

1

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19 February 2020

page(s)

15-28

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Integrated genomic analysis illustrates the central role of JAK-STAT pathway activation in myeloproliferative neoplasm pathogenesis

19 February 2020

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Improved targeting of JAK2 leads to increased therapeutic efficacy in myeloproliferative neoplasms

6 July 2018

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6 July 2018

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Somatic CALR mutations in myeloproliferative neoplasms with nonmutated JAK2

6 July 2018

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Somatic mutations of calreticulin in myeloproliferative neoplasms

6 July 2018

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Three-year efficacy, safety, and survival findings from COMFORT-II, a phase 3 study comparing ruxolitinib with best available therapy for myelofibrosis

6 July 2018

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Dual PI3K/AKT/mTOR inhibitor BEZ235 synergistically enhances the activity of JAK2 inhibitor against cultured and primary human myeloproliferative neoplasm cells

6 July 2018

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Activating CBL mutations are associated with a distinct MDS/MPN phenotype

6 July 2018

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Crystal structures of the JAK2 pseudokinase domain and the pathogenic mutant V617F

6 July 2018

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

6 July 2018

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

6 July 2018

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A double-blind, placebo-controlled trial of ruxolitinib for myelofibrosis

6 July 2018

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JAK inhibition with ruxolitinib versus best available therapy for myelofibrosis

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Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition

6 July 2018

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

6 July 2018

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

6 July 2018

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

6 July 2018

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Physiological Jak2V617F expression causes a lethal myeloproliferative neoplasm with differential effects on hematopoietic stem and progenitor cells

6 July 2018

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CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms

6 July 2018

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

6 July 2018

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6 July 2018

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6 July 2018

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A high-throughput screening for mammalian cell death effectors identifies the mitochondrial phosphate carrier as a regulator of cytochrome c release.

6 July 2018

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6 July 2018

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MPLW515L is a novel somatic activating mutation in myelofibrosis with myeloid metaplasia

6 July 2018

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Identification of an acquired JAK2 mutation in polycythemia vera

6 July 2018

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A gain-of-function mutation of JAK2 in myeloproliferative disorders

6 July 2018

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6 July 2018

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A unique clonal JAK2 mutation leading to constitutive signalling causes polycythaemia vera

6 July 2018

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Acquired mutation of the tyrosine kinase JAK2 in human myeloproliferative disorders

6 July 2018

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6 July 2018

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6 July 2018

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Autophosphorylation of JAK2 on tyrosines 221 and 570 regulates its activity

6 July 2018

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6 July 2018

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JAK1/2 and Pan-deacetylase inhibitor combination therapy yields improved efficacy in preclinical mouse models of JAK2V617F-driven disease.

6 July 2018

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Differential effects of hydroxyurea and INC424 on mutant allele burden and myeloproliferative phenotype in a JAK2-V617F polycythemia vera mouse model.

27 October 2018

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Characteristics and clinical correlates of MPL 515W>L/K mutation in essential thrombocythemia

27 October 2018

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MPL515 mutations in myeloproliferative and other myeloid disorders: a study of 1182 patients

27 October 2018

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10.1016/J.CCELL.2015.06.006

27 October 2018

Identifiers

DOI

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19 February 2020

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19 February 2020

PubMed publication ID

26175413

1 reference