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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Main Authors: Taka,T., Joonlasak,K., Huang,L., Randall Lee,T., Chang,S.W.T., Tuntiwechapikul,W.
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Published: Elsevier Limited 2015
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http://cmuir.cmu.ac.th/handle/6653943832/38184
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Institution: Chiang Mai University
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spelling 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
institution Chiang Mai University
building Chiang Mai University Library
country Thailand
collection CMU Intellectual Repository
topic Clinical Biochemistry
Drug Discovery
Pharmaceutical Science
Molecular Medicine
Molecular Biology
Organic Chemistry
Biochemistry
spellingShingle 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
description 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
publisher Elsevier Limited
publishDate 2015
url 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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