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http://dx.doi.org/10.5487/TR.2008.24.2.093

c-Jun N-Terminal Kinase Signaling Inhibitors Under Development  

Han, Sun-Young (Drug Discovery Division, Korea Research Institute of Chemical Technology)
Publication Information
Toxicological Research / v.24, no.2, 2008 , pp. 93-100 More about this Journal
Abstract
Targeting protein kinases has been active area in drug discovery. The c-Jun N-terminal kinases(JNKs) have also been target for development of novel therapy in various diseases, since the roles of JNK signaling in pathological conditions were revealed in studies using jnk-deficient mice. Small molecule inhibitors and peptide inhibitors are identified for therapeutic intervention of JNK signaling pathway. SP-600125, an anthrapyrazole small molecule inhibitor for JNK with high potency and selectivity has been widely used for dissecting JNK signaling pathway. CC-401 is the first JNK inhibitor that went into clinical trial for inflammation and leukemia. Inhibitor for mixed lineage kinase (MLK), CEP-1347 also negatively regulates JNK signaling, and tried for potential use in Parkinson's disease. Cell-permeable peptide inhibitor D-JNKI-1 is being developed for the treatment of hearing loss. The current status of these JNK inhibitors and safety issue is discussed in the minireview.
Keywords
JNK; Inhibitors; SP-600125; CC-401; AS-602801; CEP-1347; D-JNKI-1;
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