ATP non-competitive Ser/Thr kinase inhibitors as potential anticancer agents
Giorgio Cozza1, Andrea Bortolato, Ernesto Menta
1Dipartimento di Scienze Farmaceutiche, Università di Padova, Padova, Italy.
Abstract:
Protein kinases are one of the largest known families of enzyme characterized by having a well conserved ATP binding pocket. Most of the synthetic kinase inhibitors are ATP-competitive, but display some potential problems, like selectivity, discrepancy between the in vitro and in vivo inhibition assays and an high risk of developing mutation inside the ATP-binding pocket. Recently some new inhibitors with a non-competitive mechanism of action were reported, with interesting results both in vitro and in vivo.
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