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

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

  • Chem Biol. 2014 Nov 20;21(11):1433-43. doi: 10.1016/j.chembiol.2014.09.007.
Abdellah Messoussi 1,  Clémence Feneyrolles 2,  Aurélie Bros 2,  Arthur Deroide 2,  Bénédicte Daydé-Cazals 2,  Gwénaël Chevé 2,  Nathalie Van Hijfte 2,  Bénédicte Fauvel 2,  Khalid Bougrin 3,  Aziz Yasri 4
Affiliations

Affiliations

  • 1 OriBase Pharma, Cap Gamma, Parc Euromédecine, 34090 Montpellier, France; Laboratoire de Chimie des Plantes et de Synthèse Organique et Bioorganique, URAC23, Université Mohammed V-Agdal, Faculté des Sciences, B.P. 1014 Rabat, Morocco.
  • 2 OriBase Pharma, Cap Gamma, Parc Euromédecine, 34090 Montpellier, France.
  • 3 Laboratoire de Chimie des Plantes et de Synthèse Organique et Bioorganique, URAC23, Université Mohammed V-Agdal, Faculté des Sciences, B.P. 1014 Rabat, Morocco.
  • 4 OriBase Pharma, Cap Gamma, Parc Euromédecine, 34090 Montpellier, France. Electronic address: ayasri@oribase-pharma.com.
PMID: 25442375 DOI: 10.1016/j.chembiol.2014.09.007
Abstract

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.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-14761
    99.32%, JNK抑制剂
    JNK
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