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Updated: Jul 9, 2026

A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors
Published on: December 7, 2014
Targeting JAK3 tyrosine kinase-linked signal transduction pathways with rationally-designed inhibitors
Fatih M Uckun1, Alexei Vassilev, Ilker Dibirdik
1Parker Hughes Cancer Center & Parker Hughes Institute, St. Paul, MN 55113, USA. fatih_uckun@ih.org
Abstract:
Inhibitors of Janus Kinase 3 (JAK3) show potential as a new class of apoptosis-inducing anti-cancer drugs. In addition, JAK3 inhibitors may also be useful as immunosuppressive agents. Rationally designed selective inhibitors of JAK3 such as JANEX-1, that do not inhibit other Janus kinases have recently undergone extensive preclinical testing that revealed a favorable pharmacodynamic profile. Here we discuss the clinical potential of targeting JAK3-linked signal transduction pathways with small molecule inhibitors such as JANEX-1.
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