Journal
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
Volume 9, Issue 7, Pages 778-786Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/187152009789056930
Keywords
Ser/Thr kinase inhibitors; ATP non-competitive; anticancer drugs; drug discovery
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Funding
- Italian Ministry for University and Research (MIUR), Rome, Italy
- University of Padova, Padova, Italy
- European Commission [PRO-KINASERESEARCH 503467]
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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.
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