A DNA Aptameric Ligand of Human Transferrin Receptor Generated by Cell-SELEX

General cancer-targeted ligands that can deliver drugs to cells have been given considerable attention. In this paper, a high-affinity DNA aptamer (HG1) generally binding to human tumor cells was evolved by cell-SELEX, and was further optimized to have 35 deoxynucleotides (HG1-9). Aptamer HG1-9 coul...

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Main Authors: Nan Zhang, Tao Bing, Luyao Shen, Le Feng, Xiangjun Liu, Dihua Shangguan
Format: Article
Language:English
Published: MDPI AG 2021-08-01
Series:International Journal of Molecular Sciences
Subjects:
Online Access:https://www.mdpi.com/1422-0067/22/16/8923
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author Nan Zhang
Tao Bing
Luyao Shen
Le Feng
Xiangjun Liu
Dihua Shangguan
author_facet Nan Zhang
Tao Bing
Luyao Shen
Le Feng
Xiangjun Liu
Dihua Shangguan
author_sort Nan Zhang
collection DOAJ
description General cancer-targeted ligands that can deliver drugs to cells have been given considerable attention. In this paper, a high-affinity DNA aptamer (HG1) generally binding to human tumor cells was evolved by cell-SELEX, and was further optimized to have 35 deoxynucleotides (HG1-9). Aptamer HG1-9 could be taken up by live cells, and its target protein on a cell was identified to be human transferrin receptor (TfR). As a man-made ligand of TfR, aptamer HG1-9 was demonstrated to bind at the same site of human TfR as transferrin with comparable binding affinity, and was proved to cross the epithelium barrier through transferrin receptor-mediated transcytosis. These results suggest that aptamer HG1-9 holds potential as a promising ligand to develop general cancer-targeted diagnostics and therapeutics.
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spelling doaj.art-dacab00e61a2453eb66e43c4459ad3672023-11-22T08:02:39ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672021-08-012216892310.3390/ijms22168923A DNA Aptameric Ligand of Human Transferrin Receptor Generated by Cell-SELEXNan Zhang0Tao Bing1Luyao Shen2Le Feng3Xiangjun Liu4Dihua Shangguan5Beijing National Laboratory for Molecular Sciences, Key Laboratory of Analytical Chemistry for Living Biosystems, CAS Research/Education Center for Excellence in Molecular Sciences, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, ChinaBeijing National Laboratory for Molecular Sciences, Key Laboratory of Analytical Chemistry for Living Biosystems, CAS Research/Education Center for Excellence in Molecular Sciences, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, ChinaBeijing National Laboratory for Molecular Sciences, Key Laboratory of Analytical Chemistry for Living Biosystems, CAS Research/Education Center for Excellence in Molecular Sciences, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, ChinaBeijing National Laboratory for Molecular Sciences, Key Laboratory of Analytical Chemistry for Living Biosystems, CAS Research/Education Center for Excellence in Molecular Sciences, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, ChinaBeijing National Laboratory for Molecular Sciences, Key Laboratory of Analytical Chemistry for Living Biosystems, CAS Research/Education Center for Excellence in Molecular Sciences, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, ChinaBeijing National Laboratory for Molecular Sciences, Key Laboratory of Analytical Chemistry for Living Biosystems, CAS Research/Education Center for Excellence in Molecular Sciences, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, ChinaGeneral cancer-targeted ligands that can deliver drugs to cells have been given considerable attention. In this paper, a high-affinity DNA aptamer (HG1) generally binding to human tumor cells was evolved by cell-SELEX, and was further optimized to have 35 deoxynucleotides (HG1-9). Aptamer HG1-9 could be taken up by live cells, and its target protein on a cell was identified to be human transferrin receptor (TfR). As a man-made ligand of TfR, aptamer HG1-9 was demonstrated to bind at the same site of human TfR as transferrin with comparable binding affinity, and was proved to cross the epithelium barrier through transferrin receptor-mediated transcytosis. These results suggest that aptamer HG1-9 holds potential as a promising ligand to develop general cancer-targeted diagnostics and therapeutics.https://www.mdpi.com/1422-0067/22/16/8923aptameraptameric ligandcell-SELEXtransferrin receptortranscytosis
spellingShingle Nan Zhang
Tao Bing
Luyao Shen
Le Feng
Xiangjun Liu
Dihua Shangguan
A DNA Aptameric Ligand of Human Transferrin Receptor Generated by Cell-SELEX
International Journal of Molecular Sciences
aptamer
aptameric ligand
cell-SELEX
transferrin receptor
transcytosis
title A DNA Aptameric Ligand of Human Transferrin Receptor Generated by Cell-SELEX
title_full A DNA Aptameric Ligand of Human Transferrin Receptor Generated by Cell-SELEX
title_fullStr A DNA Aptameric Ligand of Human Transferrin Receptor Generated by Cell-SELEX
title_full_unstemmed A DNA Aptameric Ligand of Human Transferrin Receptor Generated by Cell-SELEX
title_short A DNA Aptameric Ligand of Human Transferrin Receptor Generated by Cell-SELEX
title_sort dna aptameric ligand of human transferrin receptor generated by cell selex
topic aptamer
aptameric ligand
cell-SELEX
transferrin receptor
transcytosis
url https://www.mdpi.com/1422-0067/22/16/8923
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