Author/Authors :
Blanco-Aparicio، نويسنده , , Carmen and Collazo، نويسنده , , Ana Marيa Garcيa and Oyarzabal، نويسنده , , Julen and Leal، نويسنده , , Juan F. and Albarلn، نويسنده , , Marيa Isabel and Lima، نويسنده , , Francisco Ramos and Pequeٌo، نويسنده , , Belén and Ajenjo، نويسنده , , Nuria and Becerra، نويسنده , , Mercedes and Alfonso، نويسنده , , Patricia and Reymundo، نويسنده , , Marيa Isabel and Palacios، نويسنده , , Irene and Mateos، نويسنده , , Genoveva and Quiٌones، نويسنده , , Helena and Corrionero، نويسنده , , Ana and Carnero، نويسنده , , Amancio and Pevarello، نويسنده , , Paolo and Lopez، نويسنده , , Ana Rodrيguez and Fominaya، نويسنده , , Jesْs and Pastor، نويسنده , , Joaquيn and Bischoff، نويسنده , , James R.، نويسنده ,
Abstract :
The serine/threonine Pim 1 kinase is an oncogene whose expression is deregulated in several human cancers. Overexpression of Pim 1 facilitates cell cycle progression and suppresses apoptosis. Hence pharmacologic inhibitors of Pim 1 are of therapeutic interest for cancer. ETP-45299 is a potent and selective inhibitor of Pim 1 that inhibits the phosphorylation of Bad and 4EBP1 in cells and suppresses the proliferation of several non-solid and solid human tumor cell lines. The combination of the PI3K inhibitor GDC-0941 with ETP-45299 was strongly synergistic in MV-4-11 AML cells, indicating that the combination of selective Pim kinase inhibitors and PI3K inhibitor could have clinical benefit.
