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.
Keywords: Ser/Thr kinase inhibitors, ATP non-competitive, anticancer drugs, drug discovery
Anti-Cancer Agents in Medicinal Chemistry
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.
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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
DOI https://dx.doi.org/10.2174/187152009789056930 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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