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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
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.
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ISSN: 0304-3835
???metadata.dc.identifier.doi???: 10.1016/j.canlet.2010.09.016
Citation: Cancer Letters 300(2): 145-153 (2011)
References: PMID: 21051136
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