| Autor: |
Gavin Bennett, Anne J. Rüger, John Thomas Feutrill, Rosemary Lynch, Ann Lewis, Anthea L. Newton, Nico Zinn, Tammy Ladduwahetty, Sunose Mihiro, Andrew Cansfield, Giovanna Bergamini, Oliver Rausch, Alan P. Watt, Douglas W. Thomson, Katie Ellard |
| Rok vydání: |
2016 |
| Předmět: |
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| Zdroj: |
ACS Medicinal Chemistry Letters. 7:768-773 |
| ISSN: |
1948-5875 |
| Popis: |
CZ415, a potent ATP-competitive mTOR inhibitor with unprecedented selectivity over any other kinase is described. In addition to a comprehensive characterization of its activities in vitro, in vitro ADME, and in vivo pharmacokinetic data are reported. The suitability of this inhibitor for studying in vivo mTOR biology is demonstrated in a mechanistic mouse model monitoring mTOR proximal downstream phosphorylation signaling. Furthermore, the compound reported here is the first ATP-competitive mTOR inhibitor described to show efficacy in a semitherapeutic collagen induced arthritis (CIA) mouse model. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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