A Small Ligand That Selectively Binds to the G-quadruplex at the Human Vascular Endothelial Growth Factor Internal Ribosomal Entry Site and Represses the Translation
G-quadruplexes are believed to have important biological functions, so many small molecules have been screened or developed for targeting G-quadruplexes. However, it is still a major challenge to find molecules that recognize specific G-quadruplexes. Here, by using a combination of surface plasmon r...
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Frontiers Media S.A.
2021
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oai:doaj.org-article:2f20155105b643479e8d937b51fb43c42021-11-09T06:29:22ZA Small Ligand That Selectively Binds to the G-quadruplex at the Human Vascular Endothelial Growth Factor Internal Ribosomal Entry Site and Represses the Translation2296-264610.3389/fchem.2021.781198https://doaj.org/article/2f20155105b643479e8d937b51fb43c42021-11-01T00:00:00Zhttps://www.frontiersin.org/articles/10.3389/fchem.2021.781198/fullhttps://doaj.org/toc/2296-2646G-quadruplexes are believed to have important biological functions, so many small molecules have been screened or developed for targeting G-quadruplexes. However, it is still a major challenge to find molecules that recognize specific G-quadruplexes. Here, by using a combination of surface plasmon resonance, electrospray ionization mass spectrometry, circular dichroism, Western blot, luciferase assay, and reverse transcriptase stop assay, we observed a small molecule, namely, oxymatrine (OMT) that could selectively bind to the RNA G-quadruplex in 5′-untranslated regions (UTRs) of human vascular endothelial growth factor (hVEGF), but could not bind to other G-quadruplexes. OMT could selectively repress the translation of VEGF in cervical cancer cells. Furthermore, it could recognize VEGF RNA G-quadruplexes in special conformations. The results indicate that OMT may serve as a potentially special tool for studying the VEGF RNA G-quadruplex in cells and as a valuable scaffold for the design of ligands that recognize different G-quadruplexes.Xiao-Xia HuXiao-Xia HuSheng-Quan WangShi-Quan GanLei LiuMing-Qing ZhongMeng-Hao JiaFei JiangYan XuChao-Da XiaoChao-Da XiaoXiang-Chun ShenXiang-Chun ShenFrontiers Media S.A.articleG-quadruplexVEGFselective ligandtranslationRNAChemistryQD1-999ENFrontiers in Chemistry, Vol 9 (2021) |
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| collection |
DOAJ |
| language |
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| topic |
G-quadruplex VEGF selective ligand translation RNA Chemistry QD1-999 |
| spellingShingle |
G-quadruplex VEGF selective ligand translation RNA Chemistry QD1-999 Xiao-Xia Hu Xiao-Xia Hu Sheng-Quan Wang Shi-Quan Gan Lei Liu Ming-Qing Zhong Meng-Hao Jia Fei Jiang Yan Xu Chao-Da Xiao Chao-Da Xiao Xiang-Chun Shen Xiang-Chun Shen A Small Ligand That Selectively Binds to the G-quadruplex at the Human Vascular Endothelial Growth Factor Internal Ribosomal Entry Site and Represses the Translation |
| description |
G-quadruplexes are believed to have important biological functions, so many small molecules have been screened or developed for targeting G-quadruplexes. However, it is still a major challenge to find molecules that recognize specific G-quadruplexes. Here, by using a combination of surface plasmon resonance, electrospray ionization mass spectrometry, circular dichroism, Western blot, luciferase assay, and reverse transcriptase stop assay, we observed a small molecule, namely, oxymatrine (OMT) that could selectively bind to the RNA G-quadruplex in 5′-untranslated regions (UTRs) of human vascular endothelial growth factor (hVEGF), but could not bind to other G-quadruplexes. OMT could selectively repress the translation of VEGF in cervical cancer cells. Furthermore, it could recognize VEGF RNA G-quadruplexes in special conformations. The results indicate that OMT may serve as a potentially special tool for studying the VEGF RNA G-quadruplex in cells and as a valuable scaffold for the design of ligands that recognize different G-quadruplexes. |
| format |
article |
| author |
Xiao-Xia Hu Xiao-Xia Hu Sheng-Quan Wang Shi-Quan Gan Lei Liu Ming-Qing Zhong Meng-Hao Jia Fei Jiang Yan Xu Chao-Da Xiao Chao-Da Xiao Xiang-Chun Shen Xiang-Chun Shen |
| author_facet |
Xiao-Xia Hu Xiao-Xia Hu Sheng-Quan Wang Shi-Quan Gan Lei Liu Ming-Qing Zhong Meng-Hao Jia Fei Jiang Yan Xu Chao-Da Xiao Chao-Da Xiao Xiang-Chun Shen Xiang-Chun Shen |
| author_sort |
Xiao-Xia Hu |
| title |
A Small Ligand That Selectively Binds to the G-quadruplex at the Human Vascular Endothelial Growth Factor Internal Ribosomal Entry Site and Represses the Translation |
| title_short |
A Small Ligand That Selectively Binds to the G-quadruplex at the Human Vascular Endothelial Growth Factor Internal Ribosomal Entry Site and Represses the Translation |
| title_full |
A Small Ligand That Selectively Binds to the G-quadruplex at the Human Vascular Endothelial Growth Factor Internal Ribosomal Entry Site and Represses the Translation |
| title_fullStr |
A Small Ligand That Selectively Binds to the G-quadruplex at the Human Vascular Endothelial Growth Factor Internal Ribosomal Entry Site and Represses the Translation |
| title_full_unstemmed |
A Small Ligand That Selectively Binds to the G-quadruplex at the Human Vascular Endothelial Growth Factor Internal Ribosomal Entry Site and Represses the Translation |
| title_sort |
small ligand that selectively binds to the g-quadruplex at the human vascular endothelial growth factor internal ribosomal entry site and represses the translation |
| publisher |
Frontiers Media S.A. |
| publishDate |
2021 |
| url |
https://doaj.org/article/2f20155105b643479e8d937b51fb43c4 |
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