Janus kinase 2 inhibition by pacritinib as potential therapeutic target for liver fibrosis. [PDF]
Background and Aims: Janus kinase 2 (JAK2) signaling is increased in human and experimental liver fibrosis with portal hypertension. JAK2 inhibitors, such as pacritinib, are already in advanced clinical development for other indications and might also be
Torres S +21 more
europepmc +3 more sources
Comprehensive kinase profile of pacritinib, a nonmyelosuppressive Janus kinase 2 inhibitor
Jack W Singer,1 Suliman Al-Fayoumi,1 Haiching Ma,2 Rami S Komrokji,3 Ruben Mesa,4 Srdan Verstovsek5 1Translational Medicine, CTI BioPharma Corp., Seattle, WA, 2Department of Research and Development, Reaction Biology, Malvern, PA, 3Department of ...
Singer J +5 more
doaj +6 more sources
Selective Janus Kinase 2 (JAK2) Pseudokinase Ligands with a Diaminotriazole Core. [PDF]
Janus kinases (JAKs) are non-receptor tyrosine kinases that are essential components of the JAK-STAT signaling pathway. Associated aberrant signaling is responsible for many forms of cancer and disorders of the immune system.
Liosi ME +8 more
europepmc +5 more sources
Distinct clinical characteristics of myeloproliferative neoplasms with calreticulin mutations [PDF]
Somatic insertions/deletions in the calreticulin gene have recently been discovered to be causative alterations in myeloproliferative neoplasms. A combination of qualitative and quantitative allele-specific polymerase chain reaction, fragment-sizing ...
Hajnalka Andrikovics +13 more
doaj +3 more sources
Functional and Structural Characterization of Clinical-Stage Janus Kinase 2 Inhibitors Identifies Determinants for Drug Selectivity. [PDF]
Janus kinase 2 (JAK2) plays a critical role in orchestrating hematopoiesis, and its deregulation leads to various blood disorders, most importantly myeloproliferative neoplasms (MPNs).
Miao Y +6 more
europepmc +2 more sources
The prolactin receptor scaffolds Janus kinase 2 via co-structure formation with phosphoinositide-4,5-bisphosphate [PDF]
Class 1 cytokine receptors transmit signals through the membrane by a single transmembrane helix to an intrinsically disordered cytoplasmic domain that lacks kinase activity. While specific binding to phosphoinositides has been reported for the prolactin
Raul Araya-Secchi +8 more
doaj +2 more sources
-escin mitigates neuroinflammation and apoptosis caused by ischemic stroke through the inhibition of the interleukin-6/Janus kinase 2/signal transducer and activator of transcription 3 signaling pathway [PDF]
Objective This study aimed to investigate the protective effects of β-escin against neuroinflammatory injury and its influence on the interleukin-6/Janus kinase 2/signal transducer and activator of transcription 3 signaling pathway in a rat model of ...
Duan Yanqin +9 more
doaj +2 more sources
Janus kinase 2 activation mechanisms revealed by analysis of suppressing mutations. [PDF]
Background Janus kinases (JAKs; JAK1 to JAK3 and tyrosine kinase 2) mediate cytokine signals in the regulation of hematopoiesis and immunity. JAK2 clinical mutations cause myeloproliferative neoplasms and leukemia, and the mutations strongly concentrate ...
Hammarén HM +5 more
europepmc +2 more sources
Janus kinase (JAK) inhibitors in the treatment of neoplastic and inflammatory disorders
The Janus kinase (JAK) family of nonreceptor protein-tyrosine kinases consists of JAK1, JAK2, JAK3, and TYK2 (Tyrosine Kinase 2). Each of these proteins contains a JAK homology pseudokinase (JH2) domain that interacts with and regulates the activity of ...
Robert Roskoski, Jr.
doaj +2 more sources
Serum amyloid A and Janus kinase 2 in a mouse model of diabetic kidney disease. [PDF]
Background Serum amyloid A (SAA), a potent inflammatory mediator, and Janus kinase 2 (JAK2), an intracellular signaling kinase, are increased by diabetes. The aims were to elucidate: 1) a JAK2-mediated pathway for increased SAA in the kidneys of diabetic
Dieter BP +9 more
europepmc +2 more sources

