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Up-regulation of Kv1.3 Channels by Janus Kinase 2
The Journal of Membrane Biology, 2015The 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
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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
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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
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Janus kinase-2 signaling mediates apoptosis in rat cardiomyocytes
Vascular Pharmacology, 2005We 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
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Janus Reveals Another Face: The Biologic Rationale for Targeting Janus Kinase 2 in Lymphoma
Journal of Clinical Oncology, 2012The 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
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An inhibitor of Janus kinase 2 prevents polycythemia in mice
Biochemical Pharmacology, 2009Polycythemia 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
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Janus kinase 2 activation participates in prostaglandin E2-induced hyperalgesia
Life Sciences, 2016Prostaglandin E2 (PGE2) is one of the major signaling molecules involved in hyperalgesia, acting directly on nociceptors and resulting in the activation of PKA and PKC. Once active, these kinases phosphorylate many cellular proteins, resulting in changes on nociceptors sensorial transduction properties.
André Schwambach, Vieira +5 more
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Modulation of Janus kinase 2 by cisplatin in cancer cells
International Journal of Oncology, 2004Constitutive 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
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Discovery of Potent and Selective Pyrazolopyrimidine Janus Kinase 2 Inhibitors
Journal of Medicinal Chemistry, 2012The 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
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Downregulation of Chloride Channel ClC-2 by Janus Kinase 3
The Journal of Membrane Biology, 2014Janus kinase-3 (JAK3) fosters proliferation and counteracts apoptosis of lymphocytes and tumor cells. The gain of function mutation (A572V)JAK3 has been discovered in acute megakaryoplastic leukemia. JAK3 is inactivated by replacement of lysine by alanine in the catalytic subunit ((K855A)JAK3).
Jamshed, Warsi +4 more
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Specific dephosphorylation of Janus Kinase 2 by protein tyrosine phosphatases
PROTEOMICS, 2014Many protein kinases are activated through phosphorylation of an activation loop thereby turning on downstream signaling pathways. Activation of JAK2, a nonreceptor tyrosine kinase with an important role in growth factor and cytokine signaling, requires phosphorylation of the 1007 and 1008 tyrosyl residues.
Jianzhuo, Li +9 more
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