Recent progress in the design, study, and development of c-Jun N-terminal kinase inhibitors as anticancer agents.

Abdellah Messoussi, Clémence Feneyrolles, Aurélie Bros, Arthur Deroide, Bénédicte Daydé-Cazals, Gwénaël Chevé, Nathalie Van Hijfte, Bénédicte Fauvel, Khalid Bougrin, Aziz Yasri

Chemistry & biology 2014 Nov 20

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The c-Jun N-terminal kinase (JNK) family, with its three members JNK1, JNK2, and JNK3, is a subfamily of mitogen-activated protein kinases. Involved in many aspects of cellular processes, JNK has been also associated with pathological states such as neurodegenerative diseases, inflammation, and cancers. In oncology, each isoform plays a distinct role depending on the context of the targeted tissue/organ, the tumor stage, and, most likely, the signaling pathway activated upstream. Consequently, the current challenge in finding new successful anti-JNK therapies is to design isoform-selective inhibitors of the JNKs. In this review, a particular focus is given to the JNK inhibitors that have been developed thus far when examining 3D structures of various JNK-inhibitor complexes. Using current data regarding structure-activity relationships and medicinal chemistry approaches, our objective is to provide a better understanding of the design and development of selective JNK inhibitors in the present and future. Copyright © 2014 Elsevier Ltd. All rights reserved.

Citation

Abdellah Messoussi, Clémence Feneyrolles, Aurélie Bros, Arthur Deroide, Bénédicte Daydé-Cazals, Gwénaël Chevé, Nathalie Van Hijfte, Bénédicte Fauvel, Khalid Bougrin, Aziz Yasri. Recent progress in the design, study, and development of c-Jun N-terminal kinase inhibitors as anticancer agents. Chemistry & biology. 2014 Nov 20;21(11):1433-43