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Selective inhibitors of the Janus Kinase Jak3 – are they effective?

Thoma, Gebhard and Drueckes, Peter and Zerwes, Hans-Guenter (2014) Selective inhibitors of the Janus Kinase Jak3 – are they effective? Bioorganic & Medicibal Chemistry Letters, 24 (19). pp. 4617-4621. ISSN 0960894X

Abstract

Jak3, together with Jak1, is involved in signal transduction initiated by several cytokines important in immune homeostasis and immune pathologies. Based on genetic evidence Jak3 has been considered to be an attractive target for immunosuppression. The approved Jak inhibitor tofacitinib (CP-690,550), originally introduced as a selective Jak3 inhibitor, also inhibited Jak1 and Jak2. The search for new selective Jak3 inhibitors has yielded several compounds whose profiles will be reviewed here. Implications on Jak3 as a therapeutic target are also discussed.

Item Type: Article
Keywords: Jak3, Jak1, Janus kinase inhibitors, Selectivity, Immunosuppression
Date Deposited: 13 Oct 2015 13:12
Last Modified: 04 Jul 2016 23:45
URI: https://oak.novartis.com/id/eprint/22912

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