Development of Akt Inhibitors
$0Z01FY2004BCNIH
Basic Sciences
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Paper 19216841Paper 18188003Paper 18000394Paper 17785575Paper 17667591Paper 17631503Paper 16546986Paper 16467077Paper 15713897Paper 15212619Paper 15087394Paper 14764993Paper 12553797
Abstract
Akt promotes cellular survival, tumorigenesis, and is activated in response to carcinogen exposure, yet the field is hampered by a lack of small molecules that directly inhibit Akt. Moreover, the lack of crystal structure of Akt has limited rational drug development. To circumvent these limitations, we have modelled Akt and have synthesized small molecules designed to specifically inhibit Akt. The goals of the project are 1. to evaluate these compounds for inhibition of Akt activity, 2. establish dose responsiveness, 3. establish specificity, 4. establish mechanism of action of inhibition, 5. establish suitability of these compounds for further development as therapeutic agents.
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