Abstract
LKB1 (also known as serine-threonine kinase 11, STK11) is a tumor suppressor, which is mutated or deleted in Peutz-Jeghers syndrome (PJS) and in a variety of cancers. Physiologically, LKB1 possesses multiple cellular functions in the regulation of cell bioenergetics metabolism, cell cycle arrest, embryo development, cell polarity, and apoptosis. New studies demonstrated that LKB1 may also play a role in the maintenance of function and dynamics of hematopoietic stem cells. Over the past years, personalized therapy targeting specific genetic aberrations has attracted intense interests. Within this review, several agents with potential activity against aberrant LKB1 signaling have been discussed. Potential strategies and challenges in targeting LKB1 inactivation are also considered.
Keywords: LKB1 (serine-threonine kinase 11, STK11), AMP-activated protein kinase (AMPK), tumor suppression, mutations, targeting therapeutics.
Current Drug Targets
Title:Targeting the LKB1 Tumor Suppressor
Volume: 15 Issue: 1
Author(s): Rui-Xun Zhao and Zhi-Xiang Xu
Affiliation:
Keywords: LKB1 (serine-threonine kinase 11, STK11), AMP-activated protein kinase (AMPK), tumor suppression, mutations, targeting therapeutics.
Abstract: LKB1 (also known as serine-threonine kinase 11, STK11) is a tumor suppressor, which is mutated or deleted in Peutz-Jeghers syndrome (PJS) and in a variety of cancers. Physiologically, LKB1 possesses multiple cellular functions in the regulation of cell bioenergetics metabolism, cell cycle arrest, embryo development, cell polarity, and apoptosis. New studies demonstrated that LKB1 may also play a role in the maintenance of function and dynamics of hematopoietic stem cells. Over the past years, personalized therapy targeting specific genetic aberrations has attracted intense interests. Within this review, several agents with potential activity against aberrant LKB1 signaling have been discussed. Potential strategies and challenges in targeting LKB1 inactivation are also considered.
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Cite this article as:
Zhao Rui-Xun and Xu Zhi-Xiang, Targeting the LKB1 Tumor Suppressor, Current Drug Targets 2014; 15 (1) . https://dx.doi.org/10.2174/1389450114666140106095811
DOI https://dx.doi.org/10.2174/1389450114666140106095811 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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