Janus kinase 3 inhibitors, also called JAK3 inhibitors, are a new class of immunomodulatory agents that inhibit Janus kinase 3. They are used for the treatment of autoimmune diseases. The Janus kinases are a family of four nonreceptor tyrosine-protein kinases, JAK1, JAK2, JAK3, and TYK2. They signal via the JAK/STAT pathway, which is important in regulating the immune system.[1] Expression of JAK3 is largely restricted to lymphocytes (predominant expression is in the hematopoietic system), while the others are ubiquitously expressed, so selective targeting of JAK3 over the other JAK isozymes is attractive as a possible treatment of autoimmune diseases.[2][3]
Activation of JAK3 by cytokine receptors that contain the common gamma chain (γc)
^Tan, Li; Akahane, Koshi; McNally, Randall; Reyskens, Kathleen M. S. E.; Ficarro, Scott B.; Liu, Suhu; Herter-Sprie, Grit S.; Koyama, Shohei; Pattison, Michael J. (2015-08-27). "Development of Selective Covalent Janus Kinase 3 Inhibitors". Journal of Medicinal Chemistry. 58 (16): 6589–6606. doi:10.1021/acs.jmedchem.5b00710. ISSN 0022-2623. PMC 4777322. PMID 26258521.
^Farmer, Luc J.; Ledeboer, Mark W.; Hoock, Thomas; Arnost, Michael J.; Bethiel, Randy S.; Bennani, Youssef L.; Black, James J.; Brummel, Christopher L.; Chakilam, Ananthsrinivas (2015-09-24). "Discovery of VX-509 (Decernotinib): A Potent and Selective Janus Kinase 3 Inhibitor for the Treatment of Autoimmune Diseases". Journal of Medicinal Chemistry. 58 (18): 7195–7216. doi:10.1021/acs.jmedchem.5b00301. ISSN 0022-2623. PMID 26230873.
^Thorarensen, Atli; Dowty, Martin E.; Banker, Mary Ellen; Juba, Brian; Jussif, Jason; Lin, Tsung; Vincent, Fabien; Czerwinski, Robert M.; Casimiro-Garcia, Agustin (2017-03-09). "Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans". Journal of Medicinal Chemistry. 60 (5): 1971–1993. doi:10.1021/acs.jmedchem.6b01694. ISSN 0022-2623. PMID 28139931.
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A Januskinaseinhibitor, also known as JAK inhibitor or jakinib, is a type of immune modulating medication, which inhibits the activity of one or more...
Januskinase3inhibitors, also called JAK3 inhibitors, are a new class of immunomodulatory agents that inhibitJanuskinase3. They are used for the treatment...
janus family of kinases. Other members of the Janus family include JAK1, JAK2 and TYK2. Januskinases (JAKs) are relatively large kinases of approximately...
the kinase activity of the first. The four JAK family members are: Januskinase 1 (JAK1) Januskinase 2 (JAK2) Januskinase3 (JAK3) Tyrosine kinase 2 (TYK2)...
Januskinase 2 (commonly called JAK2) is a non-receptor tyrosine kinase. It is a member of the Januskinase family and has been implicated in signaling...
Decernotinib is an inhibitor of Januskinase3 (JAK3) discovered through a process of inhouse screening of a chemical compound library. Decernotinib also...
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medication used for the treatment of atopic dermatitis (eczema). It is a Januskinaseinhibitor and it was developed by Pfizer. It is taken by mouth. The most common...
of cancer. It is an inhibitor of the kinases fms-like tyrosine kinase3 (FLT3), Januskinase 2 (JAK2), tropomyosin receptor kinase (trk) A (TrkA), TrkB...
who are Januskinase (JAK) inhibitor naïve or have been treated with ruxolitinib. Fedratinib acts as a competitive inhibitor of protein kinase JAK-2 with...
rheumatoid arthritis. It belongs to the class of drugs known as Januskinaseinhibitors (JAK inhibitors). Peficitinib was approved for use in Japan in 2019. Kivitz...
Ivarmacitinib (SHR0302) is a small molecule drug and selective januskinase 1 (JAK1) inhibitor. It is being developed for ulcerative colitis, eczema, alopecia...
alopecia areata (hair loss). Ritlecitinib is a kinaseinhibitor which inhibitsJanuskinase3 and tyrosine kinase. The most common side effects include headache...
juvenile idiopathic arthritis, and ulcerative colitis. It is a januskinase (JAK) inhibitor, discovered and developed by the National Institutes of Health...
with Janus family kinases (JAKs) to affect intracellular signaling. Cytokines including interleukins, interferons and hemopoietins activate the Janus kinases...
may result in cancer. Hence kinaseinhibitors such as imatinib are frequently used to treat malignancies. Januskinases are another notable example of...
kinase is Januskinase (JAK), many of whose effects are mediated by STAT proteins. (See JAK-STAT pathway.) Some kinases have dual-specificity kinase activities...
synthetic cyclohexylamino pyrrolopyrimidine januskinaseinhibitor that is relatively selective for JAK1. It inhibits signal transduction when the JAK is activated...
levels. Ruxolitinib is a Januskinaseinhibitor (JAK inhibitor) with selectivity for subtypes JAK1 and JAK2. Ruxolitinib inhibits dysregulated JAK signaling...
rheumatoid arthritis, alopecia areata, and COVID-19. It acts as an inhibitor of januskinase (JAK), blocking the subtypes JAK1 and JAK2. Baricitinib is approved...
foundation of targeted therapy. Januskinaseinhibitors, e.g. FDA approved tofacitinib ALK inhibitors, e.g. crizotinib Bcl-2 inhibitors (e.g. FDA approved venetoclax...
spondyloarthritis. Upadacitinib is a Januskinase (JAK) inhibitor that works by blocking the action of enzymes called Januskinases. These enzymes are involved...
"Selectivity Profile of the Tyrosine Kinase 2 Inhibitor Deucravacitinib Compared with JanusKinase 1/2/3Inhibitors". Dermatology and Therapy. 11 (5): 1763–1776...
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