Please use this identifier to cite or link to this item: http://hdl.handle.net/2440/95928
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Type: Journal article
Title: Targeting Mnks for cancer therapy
Author: Hou, J.
Lam, F.
Proud, C.
Wang, S.
Citation: Oncotarget, 2012; 3(2):118-131
Publisher: Impact Journals
Issue Date: 2012
ISSN: 1949-2553
1949-2553
Statement of
Responsibility: 
Jinqiang Hou, Frankie Lam, Christopher Proud and Shudong Wang
Abstract: Deregulation of protein synthesis is a common event in human cancer and a key player in translational control is eIF4E. Elevated expression levels of eIF4E promote cancer development and progression. Recent findings suggest that eIF4E activity is a key determinant of the PI3K/Akt/mTOR and Ras/Raf/MEK/ERK mediated tumorigenic activity and targeting eIF4E should have a major impact on these pathways in human cancer. The function of eIF4E is modulated through phosphorylation of a conserved serine (Ser209) by Mnk1 and Mnk2 downstream of ERK. While the phosphorylation event is necessary for oncogenic transformation, it seems to be dispensable for normal development. Hence, pharmacologic Mnk inhibitors may provide non-toxic and effective anti-cancer strategy. Strong circumstantial evidence indicates that Mnk inhibition presents attractive therapeutic potential, but the lack of selective Mnk inhibitors has so far confounded pharmacological target validation and clinical development.
Keywords: eIF4E; Mnk; Ras; Raf; MAPK; Akt; PI3K; mTOR; Targeted Cancer Therapy; Structure based drug design; Mnk Inhibitors
Rights: © 2012 Hou et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
RMID: 0030035725
DOI: 10.18632/oncotarget.453
Appears in Collections:Molecular and Biomedical Science publications

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