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The structural basis of Janus kinase 2 inhibition by a potent and specific pan-Janus kinase inhibitor

Blood, 2006
AbstractJAK2, a member of the Janus kinase (JAK) family of protein tyrosine kinases (PTKs), is an important intracellular mediator of cytokine signaling. Mutations of the JAK2 gene are associated with hematologic cancers, and aberrant JAK activity is also associated with a number of immune diseases, including rheumatoid arthritis.
Lucet, Isabelle S.   +10 more
openaire   +5 more sources

Janus kinase-1 and Janus kinase-2 inhibitors for treating myelofibrosis

2013
This is the protocol for a review and there is no abstract. The objectives are as follows: To determine the clinical efficacy and safety of JAK1 and JAK2 inhibitors for treating MF generated by hematologic or non-hematologic conditions. © 2013 The Cochrane Collaboration.
Martí-Carvajal A.J.   +3 more
openaire   +2 more sources

An inhibitor of Janus kinase 2 prevents polycythemia in mice

Biochemical Pharmacology, 2009
Polycythemia vera (PV) is a myeloproliferative disorder characterized by increased red cell mass and splenomegaly in the absence of secondary causes [Tefferi A., Spivak J.L., Polycythemia vera: scientific advances and current practice. Semin Hematol 2005;42(4):206-20.].
Anjili, Mathur   +17 more
openaire   +2 more sources

Modulation of Janus kinase 2 by cisplatin in cancer cells

International Journal of Oncology, 2004
Constitutive activation of Janus kinases (JAKs) is frequently detected in various human cancers. The activation of JAKs results in the phosphorylation and activation of signal transducers and activators of transcription (STATs). The constitutive activation of JAK/STAT pathway may play an important role in growth and survival of human cancer cells.
Hui, Song   +4 more
openaire   +2 more sources

Up-regulation of Kv1.3 Channels by Janus Kinase 2

The Journal of Membrane Biology, 2015
The janus-activated kinase 2 JAK2 participates in the signalling of several hormones including interferon, a powerful regulator of lymphocyte function. Lymphocyte activity and survival depend on the activity of the voltage-gated K(+) channel KCNA3 (Kv1.3).
Hosseinzadeh, Zohreh   +5 more
openaire   +3 more sources

Janus Reveals Another Face: The Biologic Rationale for Targeting Janus Kinase 2 in Lymphoma

Journal of Clinical Oncology, 2012
The Janus kinases (JAKs), nonreceptor protein tyrosine kinases that mediate cytokine receptor signaling, are important drivers of multiple hematologic malignancies. Canonical JAK–signal transducer and activator of transcription (STAT) signaling results in phosphorylation of STAT transcription factors, which translocate to the nucleus, bind DNA, and ...
Ann, Mullally, Benjamin L, Ebert
openaire   +2 more sources

Prolactin Promotes Hepatocellular Carcinoma through Janus Kinase 2

World Journal of Surgery, 2012
AbstractBackgroundHepatocelluar carcinoma (HCC) is one human cancer with obvious gender disparity. This study investigated the association of aberrant prolactin levels with HCC risk and the potential impacts on HCC of the prolactin receptor (PRLR)/Janus kinase 2 (JAK2) signaling.MethodsSerum prolactin of 63 HCC patients and 162 subjects without HCC was
Yao-Tsung, Yeh   +4 more
openaire   +2 more sources

Janus kinase-2 signaling mediates apoptosis in rat cardiomyocytes

Vascular Pharmacology, 2005
We tested the hypothesis that activation Jak2, which is prominently involved in the up-regulation of the renin-angiotensin system (RAS), constitutes a focal point in relaying signals triggered by a Angiotensin II (Ang II) and hypoxia/reoxygenation separately to cause an enhanced susceptibility of cardiac myocyte to apoptotic cell death.
Eduardo, Mascareno   +2 more
openaire   +2 more sources

Discovery of Potent and Selective Pyrazolopyrimidine Janus Kinase 2 Inhibitors

Journal of Medicinal Chemistry, 2012
The discovery of somatic Jak2 mutations in patients with chronic myeloproliferative neoplasms has led to significant interest in discovering selective Jak2 inhibitors for use in treating these disorders. A high-throughput screening effort identified the pyrazolo[1,5-a]pyrimidine scaffold as a potent inhibitor of Jak2.
Emily J, Hanan   +22 more
openaire   +2 more sources

Janus kinase 2 is involved in lipopolysaccharide-induced activation of macrophages

American Journal of Physiology-Cell Physiology, 2003
The mechanisms by which lipopolysaccharide (LPS) is recognized, and how such recognition leads to innate immune responses, are poorly understood. Stimulation with LPS induces the activation of a variety of proteins, including mitogen-activated protein kinases (MAPKs) and NF-κB.
Shu, Okugawa   +7 more
openaire   +2 more sources

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