Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors
CW Lindsley, Z Zhao, WH Leister, RG Robinson… - Bioorganic & medicinal …, 2005 - Elsevier
CW Lindsley, Z Zhao, WH Leister, RG Robinson, SF Barnett, D Defeo-Jones, RE Jones…
Bioorganic & medicinal chemistry letters, 2005•ElsevierThis letter describes the development of two series of potent and selective allosteric Akt
kinase inhibitors that display an unprecedented level of selectivity for either Akt1, Akt2 or
both Akt1/Akt2. An iterative analog library synthesis approach quickly provided a highly
selective Akt1/Akt2 inhibitor that induces apoptosis in tumor cells and inhibits Akt
phosphorylation in vivo.
kinase inhibitors that display an unprecedented level of selectivity for either Akt1, Akt2 or
both Akt1/Akt2. An iterative analog library synthesis approach quickly provided a highly
selective Akt1/Akt2 inhibitor that induces apoptosis in tumor cells and inhibits Akt
phosphorylation in vivo.
This letter describes the development of two series of potent and selective allosteric Akt kinase inhibitors that display an unprecedented level of selectivity for either Akt1, Akt2 or both Akt1/Akt2. An iterative analog library synthesis approach quickly provided a highly selective Akt1/Akt2 inhibitor that induces apoptosis in tumor cells and inhibits Akt phosphorylation in vivo.
Elsevier
