A Combination Strategy to Inhibit Pim-1: Synergism between Noncompetitive and ATP-Competitive Inhibitors (pages 484–496)
Dr. Mattia Mori, Dr. Cristina Tintori, Dr. Robert Selwyne Arul Christopher, Dr. Marco Radi, Prof. Silvia Schenone, Dr. Francesca Musumeci, Dr. Chiara Brullo, Dr. Patrizia Sanità, Dr. Simona Delle Monache, Dr. Adriano Angelucci, Miroslava Kissova, Dr. Emmanuele Crespan, Dr. Giovanni Maga and Prof. Maurizio Botta
Version of Record online: 22 FEB 2013 | DOI: 10.1002/cmdc.201200480
Synergism in inhibition: Through structure–activity relationship studies of known derivatives and a virtual screening campaign to identify novel compounds, ATP-competitive and noncompetitive Pim-1 inhibitors have been identified. These two classes of inhibitor exhibit a synergistic effect when tested in combination in enzymatic and cell-based assays. As such, these hits represent interesting leads for further development as anticancer agents.