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https://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. |
DOI: | 10.18632/oncotarget.453 |
Published version: | http://dx.doi.org/10.18632/oncotarget.453 |
Appears in Collections: | Aurora harvest 3 Molecular and Biomedical Science publications |
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hdl_95928.pdf | Published version | 2.76 MB | Adobe PDF | View/Open |
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