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Development of ERK5 Inhibitors for Anti-Cancer Therapy


Extracellular signal-regulated kinase 5 (ERK5) is a member of the protein kinase superfamily, which plays an essential role in the transduction of extracellular signals to intracellular effectors. Activation of the ERK5 signalling pathway is associated with cell survival, proliferation, and differentiation, and thus ERK5 over-expression may have implications in carcinogenesis. It has recently been discovered that ERK5 is also involved in the development and progression of hepatocellular carcinoma (HCC). Therefore, the discovery and development of small molecule inhibitors of ERK5 is a desirable therapeutic area.

Two potent inhibitors have been described in the literature and provide insight into the therapeutic effect caused by ERK5 inhibition and further guide our structure activity relationship studies. High throughput screening of chemical libraries conducted by Cancer Research Technology identified a number of hit compounds showing good to moderate activity. Benzo[d]thiazole and 3-cyanopyridine based inhibitors were chosen for validation by re-synthesis. The syntheses of these small libraries will be discussed.
Key references:
1. Wang, X.; Tournier, C.; Cell. Signal. 2006, 18, 753
2. Zen, K.Y.; Yasui, K.; Nakajima, T. et al. Genes, Chrom and Cancer. 2009, 48, 109-120
3. Deng, X et al. ACS Med. Chem. Lett. 2011, 2, 195-200.
4. Tatake, R. J et al. Biochem. Biophys. Res. Commun. 2008, 377, 120-125.
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