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A Janus kinase inhibitor, also known as JAK inhibitor or jakinib, [1] is a type of immune modulating medication, which inhibits the activity of one or more of the Janus kinase family of enzymes (JAK1, JAK2, JAK3, TYK2), thereby interfering with the JAK-STAT signaling pathway in lymphocytes.
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 .
[1] [4] Chemically, it is a synthetic cyclohexylamino pyrrolopyrimidine janus kinase inhibitor that is relatively selective for JAK1. [5] It inhibits signal transduction when the JAK is activated and thus helps downregulate expression of inflammatory cytokines. [medical citation needed]
Janus kinase (JAK) is a family of intracellular, non-receptor tyrosine kinases that transduce cytokine-mediated signals via the JAK-STAT pathway.They were initially named "just another kinase" 1 and 2 (since they were just two of many discoveries in a PCR-based screen of kinases), [1] but were ultimately published as "Janus kinase".
Baricitinib is a Janus kinase (JAK) inhibitor that reversibly inhibits Janus kinase 1 with a half maximal inhibitory concentration (IC 50) of 5.9 nM and Janus kinase 2 with an IC 50 of 5.7 nM. Tyrosine kinase 2, which belongs to the same enzyme family, is affected less (IC 50 = 53 nM), and Janus kinase 3 far less (IC 50 > 400 nM).
[10] [11] Upadacitinib is a Janus kinase (JAK) inhibitor that works by blocking the action of enzymes called Janus kinases. [10] [14] [11] These enzymes are involved in setting up processes that lead to inflammation, and blocking their effect brings inflammation in the joints under control. [11]
Ruxolitinib is a Janus kinase inhibitor (JAK inhibitor) with selectivity for subtypes JAK1 and JAK2. [21] [22] Ruxolitinib inhibits dysregulated JAK signaling associated with myelofibrosis. JAK1 and JAK2 recruit signal transducers and activators of transcription (STATs) to cytokine receptors leading to modulation of gene expression. [6]
CHZ868 is a drug which acts as a Janus kinase inhibitor selective for the JAK2 subtype. It was one of the first Janus kinase inhibitors developed, originally for the treatment of leukemia and related blood cancers, and while it did not get approved for clinical use, it is still used for research in the area. [1] [2] [3] [4]