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

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

Journal Name: Anti-Cancer Agents in Medicinal Chemistry
(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Volume 9 , Issue 7 , 2009

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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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Article Details

Year: 2009
Page: [778 - 786]
Pages: 9
DOI: 10.2174/187152009789056930
Price: $65

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