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Please use this identifier to cite or link to this item: http://hdl.handle.net/10261/38835
Title: 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
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
DOI: 10.1016/j.canlet.2010.09.016
ISSN: 0304-3835
References: PMID: 21051136
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