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Closed Access item Pim 1 kinase inhibitor ETP-45299 suppresses cellular proliferation and synergizes with PI3K inhibition

Authors:Blanco-Aparicio, Carmen
García Collazo, Ana María
Oyarzabal, Julen
Leal, Juan F. M.
Albarrán, María Isabel
Ramos Lima, Francisco
Pequeño, Belén
Ajenjo, Nuria
Becerra, Mercedes
Alfonso, Patricia
Reymundo, María Isabel
Palacios, Irene
Mateos, Genoveva
Quiñones, Helena
Corrionero, Ana
Carnero, Amancio
Pevarello, Paolo
Rodríguez López, Ana
Fominaya, Jesús
Pastor, Joaquín
Bischoff, James R.
Keywords:Pim 1, Kinase inhibitors, PI3K, AML
Issue Date:3-Nov-2010
Publisher:Elsevier
Citation:Cancer Letters 300(2): 145-153 (2011)
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.
Description:9 páginas, 4 figuras, 2 tablas.
Publisher version (URL):http://dx.doi.org/10.1016/j.canlet.2010.09.016
URI:http://hdl.handle.net/10261/38835
ISSN:0304-3835
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