Janus kinase inhibitor

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.

It is used in the treatment of cancer and inflammatory diseases[1][2] such as rheumatoid arthritis[3] and various skin conditions.[4] A Janus kinase 3 inhibitor is attractive as a possible treatment of various autoimmune diseases since its function is mainly restricted to lymphocytes. As of 2017, development of a selective JAK3 inhibitor was ongoing.[5]

  1. ^ a b Kontzias A, Kotlyar A, Laurence A, Changelian P, O'Shea JJ (August 2012). "Jakinibs: a new class of kinase inhibitors in cancer and autoimmune disease". Current Opinion in Pharmacology. 12 (4): 464–70. doi:10.1016/j.coph.2012.06.008. PMC 3419278. PMID 22819198.
  2. ^ Pesu M, Laurence A, Kishore N, Zwillich SH, Chan G, O'Shea JJ (June 2008). "Therapeutic targeting of Janus kinases". Immunological Reviews. 223: 132–42. doi:10.1111/j.1600-065X.2008.00644.x. PMC 2634846. PMID 18613833.
  3. ^ Norman P (August 2014). "Selective JAK inhibitors in development for rheumatoid arthritis". Expert Opinion on Investigational Drugs. 23 (8): 1067–77. doi:10.1517/13543784.2014.918604. PMID 24818516. S2CID 21143324.
  4. ^ "JAK Inhibitors Showing Promise for Many Skin Problems - Conditions ranging from alopecia to vitiligo". 6 July 2017. Archived from the original on 13 July 2017. Retrieved 9 July 2017.
  5. ^ Forster M, Gehringer M, Laufer SA (September 2017). "Recent advances in JAK3 inhibition: Isoform selectivity by covalent cysteine targeting". Bioorganic & Medicinal Chemistry Letters. 27 (18): 4229–4237. doi:10.1016/j.bmcl.2017.07.079. PMID 28844493.