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Anti-Cancer Agents in Medicinal Chemistry


ISSN (Print): 1871-5206
ISSN (Online): 1875-5992

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

Author(s): Giorgio Cozza, Andrea Bortolato, Ernesto Menta, Ennio Cavalletti, Silvano Spinelli and Stefano Moro

Volume 9, Issue 7, 2009

Page: [778 - 786] Pages: 9

DOI: 10.2174/187152009789056930

Price: $65


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.

Keywords: Ser/Thr kinase inhibitors, ATP non-competitive, anticancer drugs, drug discovery

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