ATP Non-Competitive Ser/Thr Kinase Inhibitors as Potential Anticancer Agents

作者：Cozza Giorgio; Bortolato Andrea; Menta Ernesto; Cavalletti Ennio; Spinelli Silvano; Moro Stefano^*

来源：Anti-Cancer Agents in Medicinal Chemistry, 2009, 9(7): 778-786.

DOI：10.2174/187152009789056930

• Ser/Thr kinase inhibitors
• ATP non-competitive
• anticancer drugs
• drug discovery

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.

• 出版日期2009-9