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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

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   +3 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

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

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

Janus kinase 2 activation participates in prostaglandin E2-induced hyperalgesia

Life Sciences, 2016
Prostaglandin 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
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

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

Downregulation of Chloride Channel ClC-2 by Janus Kinase 3

The Journal of Membrane Biology, 2014
Janus 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
openaire   +2 more sources

Specific dephosphorylation of Janus Kinase 2 by protein tyrosine phosphatases

PROTEOMICS, 2014
Many 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
openaire   +2 more sources

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