<it>In vitro </it>anti-angiogenic properties of LGD1069, a selective retinoid X-receptor agonist through down-regulating Runx2 expression on Human endothelial cells

<p>Abstract</p> <p>Background</p> <p>LGD1069 (Targretin<sup>®</sup>) is a selective retinoid X receptor (RXR) ligand, which is used in patients for cutaneous T-cell lymphoma. Our published study reported that LGD1069 inhibited tumor-induced angiogenesis in n...

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Main Authors: Lu Hong, Liu Yu-Hui, Wang Wei, Fu Jianjiang, Luo Yongming
Format: Article
Language:English
Published: BMC 2011-06-01
Series:BMC Cancer
Subjects:
Online Access:http://www.biomedcentral.com/1471-2407/11/227
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author Lu Hong
Liu Yu-Hui
Wang Wei
Fu Jianjiang
Luo Yongming
author_facet Lu Hong
Liu Yu-Hui
Wang Wei
Fu Jianjiang
Luo Yongming
author_sort Lu Hong
collection DOAJ
description <p>Abstract</p> <p>Background</p> <p>LGD1069 (Targretin<sup>®</sup>) is a selective retinoid X receptor (RXR) ligand, which is used in patients for cutaneous T-cell lymphoma. Our published study reported that LGD1069 inhibited tumor-induced angiogenesis in non-small cell lung cancer. In present study, we found that LGD1069 suppressed the proliferation, adhesion, invasion and migration of endothelial cells directly, and affected the expression of vegf and some matrix genes.</p> <p>Methods</p> <p>Human umbilical vein endothelial cells (HUVECs) were used for <it>in vitro </it>study. MTT assay and Sulforhodamine B assay were used for cell viability assay; the tube formation assay was used to investigate the effect of LGD1069 on angiogenesis <it>in vitro</it>. <it>In vitro </it>adhesion, migration and invasion of HUVEC cells were analyzed by Matrigel adhesion, migration and invasion assay. Gene expressions were measured by RT-PCR and Western blot analysis.</p> <p>Results</p> <p>Our data showed here that LGD1069 inhibited the activation of TGF-β/Smad pathway significantly. Furthermore, it was demonstrated that expression of Runx2 was suppressed pronouncedly during incubation with LGD1069. Runx2 is a DNA-binding transcription factor which plays a master role in tumor-induced angiogenesis and cancer cells metastasis by interaction with the TGF-β/Smad pathway of transcriptional modulators.</p> <p>Conclusions</p> <p>Our results suggested that LGD1069 may impair angiogenic and metastatic potential induced by tumor cells through suppressing expression of Runx2 directly on human endothelial cells, which may point out new pathway through which LGD1069 display anti-angiogenic properties, and provide new molecular evidence to support LGD1069 as a potent anti-metastatic agent in cancer therapy.</p>
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spelling doaj.art-f3eaeb6b198f46eab5be8436407b1c982022-12-21T21:04:52ZengBMCBMC Cancer1471-24072011-06-0111122710.1186/1471-2407-11-227<it>In vitro </it>anti-angiogenic properties of LGD1069, a selective retinoid X-receptor agonist through down-regulating Runx2 expression on Human endothelial cellsLu HongLiu Yu-HuiWang WeiFu JianjiangLuo Yongming<p>Abstract</p> <p>Background</p> <p>LGD1069 (Targretin<sup>®</sup>) is a selective retinoid X receptor (RXR) ligand, which is used in patients for cutaneous T-cell lymphoma. Our published study reported that LGD1069 inhibited tumor-induced angiogenesis in non-small cell lung cancer. In present study, we found that LGD1069 suppressed the proliferation, adhesion, invasion and migration of endothelial cells directly, and affected the expression of vegf and some matrix genes.</p> <p>Methods</p> <p>Human umbilical vein endothelial cells (HUVECs) were used for <it>in vitro </it>study. MTT assay and Sulforhodamine B assay were used for cell viability assay; the tube formation assay was used to investigate the effect of LGD1069 on angiogenesis <it>in vitro</it>. <it>In vitro </it>adhesion, migration and invasion of HUVEC cells were analyzed by Matrigel adhesion, migration and invasion assay. Gene expressions were measured by RT-PCR and Western blot analysis.</p> <p>Results</p> <p>Our data showed here that LGD1069 inhibited the activation of TGF-β/Smad pathway significantly. Furthermore, it was demonstrated that expression of Runx2 was suppressed pronouncedly during incubation with LGD1069. Runx2 is a DNA-binding transcription factor which plays a master role in tumor-induced angiogenesis and cancer cells metastasis by interaction with the TGF-β/Smad pathway of transcriptional modulators.</p> <p>Conclusions</p> <p>Our results suggested that LGD1069 may impair angiogenic and metastatic potential induced by tumor cells through suppressing expression of Runx2 directly on human endothelial cells, which may point out new pathway through which LGD1069 display anti-angiogenic properties, and provide new molecular evidence to support LGD1069 as a potent anti-metastatic agent in cancer therapy.</p>http://www.biomedcentral.com/1471-2407/11/227LGD1069retinoid X receptormetastasisangiogenesisRunx2
spellingShingle Lu Hong
Liu Yu-Hui
Wang Wei
Fu Jianjiang
Luo Yongming
<it>In vitro </it>anti-angiogenic properties of LGD1069, a selective retinoid X-receptor agonist through down-regulating Runx2 expression on Human endothelial cells
BMC Cancer
LGD1069
retinoid X receptor
metastasis
angiogenesis
Runx2
title <it>In vitro </it>anti-angiogenic properties of LGD1069, a selective retinoid X-receptor agonist through down-regulating Runx2 expression on Human endothelial cells
title_full <it>In vitro </it>anti-angiogenic properties of LGD1069, a selective retinoid X-receptor agonist through down-regulating Runx2 expression on Human endothelial cells
title_fullStr <it>In vitro </it>anti-angiogenic properties of LGD1069, a selective retinoid X-receptor agonist through down-regulating Runx2 expression on Human endothelial cells
title_full_unstemmed <it>In vitro </it>anti-angiogenic properties of LGD1069, a selective retinoid X-receptor agonist through down-regulating Runx2 expression on Human endothelial cells
title_short <it>In vitro </it>anti-angiogenic properties of LGD1069, a selective retinoid X-receptor agonist through down-regulating Runx2 expression on Human endothelial cells
title_sort it in vitro it anti angiogenic properties of lgd1069 a selective retinoid x receptor agonist through down regulating runx2 expression on human endothelial cells
topic LGD1069
retinoid X receptor
metastasis
angiogenesis
Runx2
url http://www.biomedcentral.com/1471-2407/11/227
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