Discovery of Potent and Selective MRCK Inhibitors with Therapeutic Effect on Skin Cancer

The myotonic dystrophy-related Cdc42-binding kinases MRCKα and MRCKβ contribute to the regulation of actin-myosin cytoskeleton organization and dynamics, acting in concert with the Rho-associated coiled-coil kinases ROCK1 and ROCK2. The absence of highly potent and selective MRCK inhibitors has resu...

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Veröffentlicht in:	Cancer research (Chicago, Ill.) Ill.), 2018-04, Vol.78 (8), p.2096-2114
Hauptverfasser:	Unbekandt, Mathieu, Belshaw, Simone, Bower, Justin, Clarke, Maeve, Cordes, Jacqueline, Crighton, Diane, Croft, Daniel R, Drysdale, Martin J, Garnett, Mathew J, Gill, Kathryn, Gray, Christopher, Greenhalgh, David A, Hall, James A M, Konczal, Jennifer, Lilla, Sergio, McArthur, Duncan, McConnell, Patricia, McDonald, Laura, McGarry, Lynn, McKinnon, Heather, McMenemy, Carol, Mezna, Mokdad, Morrice, Nicolas A, Munro, June, Naylor, Gregory, Rath, Nicola, Schüttelkopf, Alexander W, Sime, Mairi, Olson, Michael F
Format:	Artikel
Sprache:	eng
Schlagworte:	Actin Animals Antineoplastic Agents - pharmacology Antineoplastic Agents - therapeutic use Blood cancer Cancer Carcinogenesis Carcinoma, Squamous Cell - drug therapy Carcinoma, Squamous Cell - enzymology Cdc42 protein Cell Line, Tumor Cell migration Cytoskeleton Disease Models, Animal Drug Discovery Dystrophy HEK293 Cells Humans Inhibitors Invasiveness Mass spectrometry Mass spectroscopy Mice Mice, Nude Myosin Myotonic dystrophy Myotonin-Protein Kinase - antagonists & inhibitors Papilloma Pharmacodynamics Phosphorylation Protein Kinase Inhibitors - pharmacology Protein Kinase Inhibitors - therapeutic use Pyridines - pharmacology Pyridines - therapeutic use Pyrimidines - pharmacology Pyrimidines - therapeutic use Pyrroles - pharmacology Pyrroles - therapeutic use Skin cancer Skin Neoplasms - drug therapy Skin Neoplasms - enzymology Squamous cell carcinoma Substrate inhibition Tumor cell lines Xenograft Model Antitumor Assays
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