c-Jun N-Terminal Kinase (JNK/SAP Kinase) Inhibitors
Jun N-terminal kinase (JNK), a serine-directed protein kinase, is involved in the phosphorylation and activation of c-Jun and ATF2 and plays a significant role in metabolism, growth, cell differentiation, apoptosis, and participates in stress responses, such as those induced by hypoxin, cold shock, and hyperosmolarity. The three isoforms of JNK, known as JNK1, 2, and 3, are encoded by 3, independent genes. They phosphorylate Ser63 and Ser73 at the region of c-Jun and enhance its transcriptional activity. JNK1 and 2 exhibit broad tissue expression profiles. In contrast, JNK3 is expressed predominantly in the central nervous system. JNK is activated in response to inflammation, endotoxins, and environmental stress. Its activation can mediate proinflammatory gene expression, cell proliferation and apoptosis.
