Title: ATP Non-Competitive Ser/Thr Kinase Inhibitors as Potential Anticancer Agents
Volume: 9
Issue: 7
Author(s): Giorgio Cozza, Andrea Bortolato, Ernesto Menta, Ennio Cavalletti, Silvano Spinelli and Stefano Moro
Affiliation:
Keywords:
Ser/Thr kinase inhibitors, ATP non-competitive, anticancer drugs, drug discovery
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 intresting results both in vitro and in vivo.
