Article
Modulating Protein-Protein Interactions of the Mitotic Polo-like Kinases to Target Mutant KRAS.
Cell chemical biology - 17 Aug 2017
Narvaez Ana J, Ber Suzan, Crooks Alex, Emery Amy, Hardwick Bryn, Guarino Almeida Estrella, Huggins David J, Perera David, Roberts-Thomson Meredith, Azzarelli Roberta, Hood Fiona E, Prior Ian A, Walker David W, Boyce Richard, Boyle Robert G, Barker Samuel P, Torrance Christopher J, McKenzie Grahame J, Venkitaraman Ashok R
Abstract excerpt
Mutations activating KRAS underlie many forms of cancer, but are refractory to therapeutic targeting. Here, we develop Poloppin, an inhibitor of protein-protein interactions via the Polo-box domain (PBD) of the mitotic Polo-like kinases (PLKs), in monotherapeutic and combination strategies to target mutant KRAS. Poloppin engages its targets in biochemical and cellular assays, triggering mitotic arrest with...
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