A novel small-molecule MRCK inhibitor blocks cancer cell invasion.
Unbekandt, M., Croft, D.R., Crighton, D., Mezna, M., McArthur, D., McConnell, P., Schuttelkopf, A.W., Belshaw, S., Pannifer, A., Sime, M., Bower, J., Drysdale, M., Olson, M.F.(2014) Cell Commun Signal 12: 54-54
- PubMed: 25288205 
- DOI: https://doi.org/10.1186/s12964-014-0054-x
- Primary Citation of Related Structures:  
4UAK, 4UAL - PubMed Abstract: 
The myotonic dystrophy kinase-related CDC42-binding kinases MRCKα and MRCKβ regulate actin-myosin contractility and have been implicated in cancer metastasis. Along with the related ROCK1 and ROCK2 kinases, the MRCK proteins initiate signalling events that lead to contractile force generation which powers cancer cell motility and invasion. A potential strategy for cancer therapy is to reduce metastasis by blocking MRCK activity, either alone or in combination with ROCK inhibition. However, to date no potent small molecule inhibitors have been developed with selectivity towards MRCK.