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Covalent Janus Kinase 3 Inhibitors

2020
During 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
openaire   +1 more source

[Janus kinase inhibitors].

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 ...
openaire   +1 more source

Comparative safety of Janus kinase inhibitors and tumor necrosis factor inhibitors in patients undergoing treatment for rheumatoid arthritis

International Journal of Rheumatic Diseases, 2022
Since 2010, biological disease‐modifying antirheumatic drugs (bDMARDs) have been the dominant mode of treatment for rheumatoid arthritis (RA). However, the safety of DMARDs, such as tumor necrosis factor inhibitors (TNFis) and Janus kinase inhibitors ...
Yao-Fan Fang   +4 more
semanticscholar   +1 more source

Selective Janus kinase inhibitors come of age

Nature Reviews Rheumatology, 2019
Janus 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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Systematic review of newer agents for the management of alopecia areata in adults: Janus kinase inhibitors, biologics and phosphodiesterase‐4 inhibitors

Journal of the European Academy of Dermatology and Venereology, 2022
Management options for moderate‐to‐severe alopecia areata (AA) are limited owing to a lack of safe and effective treatments suitable for long‐term use.
Aditya K. Gupta   +5 more
semanticscholar   +1 more source

[Janus kinase inhibitors].

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
openaire   +1 more source

Janus Kinase Inhibitors and Non-Melanoma Skin Cancer

Current Treatment Options in Oncology, 2021
JAK (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
openaire   +2 more sources

Dehydrocrenatidine Is a Novel Janus Kinase Inhibitor

Molecular Pharmacology, 2015
Janus 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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Janus kinase inhibitors role in bone remodeling

Journal of Cellular Physiology, 2019
AbstractJanus kinases (JAKs) play a pleiotropic role in several important physiological processes, such as cell maturation, cell proliferation, and cell death, via providing transmission signals from several molecules, such as cytokines, interferons, hormones, and growth factors, to the nucleus. Bone physiology and remodeling are markedly influenced by
Nicola Maruotti   +3 more
openaire   +3 more sources

Janus kinase inhibitors for rheumatoid arthritis

Current Opinion in Chemical Biology, 2016
Treatment of autoimmune diseases, such as rheumatoid arthritis (RA), has advanced substantially over the past decade with the development of biologics targeting inflammatory cytokines. Recent progress in treating RA has been achieved with janus kinase (JAK) inhibitors (Jakinibs), an orally available disease-modifying anti-rheumatic drug targeting the ...
openaire   +2 more sources

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