Results 311 to 320 of about 83,254 (357)
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2017
To control gene expression, cytokines and other extracellular molecules utilize the Janus kinase (JAK) and signal transducers and activators of transcription (STAT). Dysregulation of the JAK-STAT pathway has been implicated in a myriad of inflammatory and hematologic disorders.
Andrew Kim, Bruce Strober
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To control gene expression, cytokines and other extracellular molecules utilize the Janus kinase (JAK) and signal transducers and activators of transcription (STAT). Dysregulation of the JAK-STAT pathway has been implicated in a myriad of inflammatory and hematologic disorders.
Andrew Kim, Bruce Strober
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[Pharmacology of Janus kinase inhibitors].
Der Hautarzt; Zeitschrift fur Dermatologie, Venerologie, und verwandte Gebiete, 2019Modern dermatotherapy is dominated by the development of various biologicals and small molecules. Janus kinase inhibitors (JAKi) form a novel class of small molecular synthetic compounds inhibiting the intracellular signal transduction of cytokine receptors. Cytokines are key mediators in the pathophysiology of numerous inflammatory skin diseases. Many
F, Solimani, F J, Hilke, K, Ghoreschi
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Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs)
Bioorganic & Medicinal Chemistry Letters, 2009A series of phenylaminopyrimidines has been identified as inhibitors of Janus kinases (JAKs). Development of this initial series led to the potent JAK2/JAK1 inhibitor CYT387 (N-(cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]-benzamide). Details of synthesis and SAR studies of these compounds are reported.
Burns, Christopher J. +22 more
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Covalent Janus Kinase 3 Inhibitors
2020During the past decade, covalent targeting has experienced a revival, especially in the kinase field. Addressing non-conserved cysteine residues by targeted covalent inhibitors has enabled the design of ligands with high selectivity in the kinome and has led to five currently approved drugs (1–5; early September 2018).
Matthias Gehringer, Michael Forster
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Zeitschrift fur Rheumatologie, 2022
In 2017 the first Janus kinase (JAK) inhibitors were approved for the treatment of rheumatoid arthritis in Germany. The mode of action of JAK inhibitors differs from biologicals, as multiple cytokines are inhibited. In comparison with the treatment with biologicals, JAK inhibitors have the advantage of oral application, three of the four currently ...
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In 2017 the first Janus kinase (JAK) inhibitors were approved for the treatment of rheumatoid arthritis in Germany. The mode of action of JAK inhibitors differs from biologicals, as multiple cytokines are inhibited. In comparison with the treatment with biologicals, JAK inhibitors have the advantage of oral application, three of the four currently ...
openaire +1 more source
Selective Janus kinase inhibitors come of age
Nature Reviews Rheumatology, 2019Janus kinase (JAK) inhibitors (jakinibs) that target downstream signalling by a large range of cytokines are effective in treating autoimmune and rheumatic diseases. Newer jakinibs that selectively inhibit individual JAKs and a narrower spectrum of cytokines have now been developed, but how do these inhibitors compare with existing drugs?
John J, O'Shea, Massimo, Gadina
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Efficacy of Janus kinase inhibitors in rheumatoid arthritis
Inflammation Research, 2023Janus kinase inhibitors (JAKis) is a new therapeutic class in autoimmune and inflammatory diseases. Four molecules are approved in rheumatoid arthritis (RA) in Europe. Recently, questions have raised about adverse events. In this context, a synthesis of the efficacy data of JAKis in RA is of use.We performed a literature review based on published ...
Camille, Langbour +3 more
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Zeitschrift fur Rheumatologie, 2013
Janus protein tyrosine kinase (JAK) inhibitors are new therapeutic targets in the treatment of rheumatoid arthritis. Tofacitinib has shown good clinical efficacy in phase II and III studies with American College of Rheumatology (ACR) 20 response rates over 50% for monotherapy and in combination with methotrexate (MTX).
E, Ostermeier, P, Roll, H-P, Tony
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Janus protein tyrosine kinase (JAK) inhibitors are new therapeutic targets in the treatment of rheumatoid arthritis. Tofacitinib has shown good clinical efficacy in phase II and III studies with American College of Rheumatology (ACR) 20 response rates over 50% for monotherapy and in combination with methotrexate (MTX).
E, Ostermeier, P, Roll, H-P, Tony
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Janus Kinase Inhibitors and Non-Melanoma Skin Cancer
Current Treatment Options in Oncology, 2021JAK (janus kinase) inhibitors are becoming increasingly prescribed for various conditions from dermatologic diseases to graft versus host disease in bone marrow transplant recipients. This class of drugs has been found to be truly life-changing for many, though they are not without potential adverse effects.
Charlotte S, Greif +2 more
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Dehydrocrenatidine Is a Novel Janus Kinase Inhibitor
Molecular Pharmacology, 2015Janus kinase (JAK) 2 plays a pivotal role in the tumorigenesis of signal transducers and activators of transcription (STAT) 3 constitutively activated solid tumors. JAK2 mutations are involved in the pathogenesis of various types of hematopoietic disorders, such as myeloproliferative disorders, polycythemia vera, essential thrombocythemia, and primary ...
Jing, Zhang +10 more
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