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

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.

Cite this article as:

Cozza Giorgio, Bortolato Andrea, Menta Ernesto, Cavalletti Ennio, Spinelli Silvano and Moro Stefano, ATP Non-Competitive Ser/Thr Kinase Inhibitors as Potential Anticancer Agents, Anti-Cancer Agents in Medicinal Chemistry 2009; 9(7) . https://dx.doi.org/10.2174/187152009789056930