ATP-competitive Inhibitors Block Protein Kinase Recruitment to the Hsp90-Cdc37 System

Polier, S, et al., 9(5), 307-12, Nat Chem Biol, 2013

Authors demonstrate that Cdc37 directly antagonizes ATP binding to client protein kinases and inhibits phosphorylation of kinase substrates. ATP-competitive inhibitors are also shown to antagonize Cdc37 interaction with Hsp90-dependent kinases in vitro.The binding of Cdc37 to B-Raf protein kinase domain in the presence of ATP-competitive kinase inhibitors was assessed on the Octet RED96 system using Anti-Penta-HIS biosensors.

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