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JNK, p38, ERK, and SGK1 Inhibitors in Cancer
Jonas Cicenas1,2,3, Egle Zalyte4, Arnas Rimkus5
1Department for Microbiology, Immunbiology und Genetics, Max F. Perutz Laboratories, University of Vienna, Vienna AT-1030, Austria. j.cicenas@mapkinases.eu.
Abstract:
Mitogen-activated protein kinases (MAP kinases) are a family of kinases that regulates a range of biological processes implicated in the response to growth factors like latelet-derived growth factor (PDGF), epidermal growth factor (EGF), vascular endothelial growth factor (VEGF), and stress, such as ultraviolet irradiation, heat shock, and osmotic shock. The MAP kinase family consists of four major subfamilies of related proteins (extracellular regulated kinases 1/2 (ERK1/2), c-Jun N-terminal kinase (JNK), p38, and extracellular regulated kinase 5 (ERK5)) and regulates numerous cellular activities, such as apoptosis, gene expression, mitosis, differentiation, and immune responses. The deregulation of these kinases is shown to be involved in human diseases, such as cancer, immune diseases, inflammation, and neurodegenerative disorders. The awareness of the therapeutic potential of the inhibition of MAP kinases led to a thorough search for small-molecule inhibitors. Here, we discuss some of the most well-known MAP kinase inhibitors and their use in cancer research.
Insights
Mitogen-activated protein (MAP) kinases regulate vital cellular functions and are implicated in diseases like cancer. This review highlights key MAP kinase inhibitors and their application in cancer research.
Area of Science:
- Biochemistry
- Cell Biology
Background:
- Mitogen-activated protein (MAP) kinases are crucial signaling proteins regulating cellular responses to growth factors and stress.
- The MAP kinase family includes ERK1/2, JNK, p38, and ERK5, controlling apoptosis, gene expression, mitosis, differentiation, and immune responses.
Discussion:
- Dysregulation of MAP kinases is linked to human diseases, including cancer, inflammation, immune disorders, and neurodegeneration.
- Targeting MAP kinases therapeutically is a significant focus in drug discovery.
Key Insights:
- Small-molecule inhibitors targeting MAP kinases are actively being developed.
- These inhibitors hold promise for treating various cancers.
Outlook:
- Further research into MAP kinase inhibitors is essential for advancing cancer therapies.
- Understanding these pathways can lead to novel therapeutic strategies for complex diseases.
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