Targeting JAK3 tyrosine kinase-linked signal transduction pathways with rationally-designed inhibitors.
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.
Uckun
Fatih M
FM
Parker Hughes Cancer Center & Parker Hughes Institute, St. Paul, MN 55113, USA. fatih_uckun@ih.org
Vassilev
Alexei
A
Dibirdik
Ilker
I
Tibbles
Heather
H
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D004195:Disease Models, Animal; D015195:Drug Design; D006801:Humans; D007166:Immunosuppressive Agents / Q000737:chemistry; D053616:Janus Kinase 3 / Q000037:antagonists & inhibitors* / Q000187:drug effects; D015398:Signal Transduction / Q000187:drug effects*; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D007166:Immunosuppressive Agents; D053616:Janus Kinase 3