Down-regulation of the human VEGF gene expression by perylene monoimide derivatives
The proximal promoter region of the human vascular endothelial growth factor (VEGF) gene contains a guanine-rich strand that can act as a transcriptional silencer by forming an intramolecular G-quadruplex. In this study, we compared two perylene monoimide derivatives, PM1 and PM2, with the well-stud...
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th-cmuir.6653943832-381842015-06-16T07:46:31Z Down-regulation of the human VEGF gene expression by perylene monoimide derivatives Taka,T. Joonlasak,K. Huang,L. Randall Lee,T. Chang,S.W.T. Tuntiwechapikul,W. Clinical Biochemistry Drug Discovery Pharmaceutical Science Molecular Medicine Molecular Biology Organic Chemistry Biochemistry The proximal promoter region of the human vascular endothelial growth factor (VEGF) gene contains a guanine-rich strand that can act as a transcriptional silencer by forming an intramolecular G-quadruplex. In this study, we compared two perylene monoimide derivatives, PM1 and PM2, with the well-studied perylene diimide derivative, PIPER, and the well-studied porphyrin derivative, TmPyP 4, with regard to G-quadruplex formation, G-quadruplex binding selectivity, and human VEGF gene silencing in A549 lung cancer cells. The results show that these perylene derivatives can preferentially induce intramolecular G-quadruplex formation from a duplex containing the VEGF G-quadruplex motif in vitro. Incubating A549 lung cancer cells with these perylene derivatives, especially PM2, led to the reduction of both VEGF mRNA and VEGF protein. This study might provide the foundation for the rational design and development of new perylene derivatives as effective anti-angiogenesis agents for cancer therapy. © 2011 Elsevier Ltd. All rights reserved. 2015-06-16T07:46:31Z 2015-06-16T07:46:31Z 2012-01-01 Article 0960894X 2-s2.0-84655169275 10.1016/j.bmcl.2011.10.089 22104143 http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84655169275&origin=inward http://cmuir.cmu.ac.th/handle/6653943832/38184 Elsevier Limited |
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Clinical Biochemistry Drug Discovery Pharmaceutical Science Molecular Medicine Molecular Biology Organic Chemistry Biochemistry Taka,T. Joonlasak,K. Huang,L. Randall Lee,T. Chang,S.W.T. Tuntiwechapikul,W. Down-regulation of the human VEGF gene expression by perylene monoimide derivatives |
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The proximal promoter region of the human vascular endothelial growth factor (VEGF) gene contains a guanine-rich strand that can act as a transcriptional silencer by forming an intramolecular G-quadruplex. In this study, we compared two perylene monoimide derivatives, PM1 and PM2, with the well-studied perylene diimide derivative, PIPER, and the well-studied porphyrin derivative, TmPyP 4, with regard to G-quadruplex formation, G-quadruplex binding selectivity, and human VEGF gene silencing in A549 lung cancer cells. The results show that these perylene derivatives can preferentially induce intramolecular G-quadruplex formation from a duplex containing the VEGF G-quadruplex motif in vitro. Incubating A549 lung cancer cells with these perylene derivatives, especially PM2, led to the reduction of both VEGF mRNA and VEGF protein. This study might provide the foundation for the rational design and development of new perylene derivatives as effective anti-angiogenesis agents for cancer therapy. © 2011 Elsevier Ltd. All rights reserved. |
format |
Article |
author |
Taka,T. Joonlasak,K. Huang,L. Randall Lee,T. Chang,S.W.T. Tuntiwechapikul,W. |
author_facet |
Taka,T. Joonlasak,K. Huang,L. Randall Lee,T. Chang,S.W.T. Tuntiwechapikul,W. |
author_sort |
Taka,T. |
title |
Down-regulation of the human VEGF gene expression by perylene monoimide derivatives |
title_short |
Down-regulation of the human VEGF gene expression by perylene monoimide derivatives |
title_full |
Down-regulation of the human VEGF gene expression by perylene monoimide derivatives |
title_fullStr |
Down-regulation of the human VEGF gene expression by perylene monoimide derivatives |
title_full_unstemmed |
Down-regulation of the human VEGF gene expression by perylene monoimide derivatives |
title_sort |
down-regulation of the human vegf gene expression by perylene monoimide derivatives |
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Elsevier Limited |
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2015 |
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http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84655169275&origin=inward http://cmuir.cmu.ac.th/handle/6653943832/38184 |
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