title: Study of the Function of G-Rich Aptamers Selected for Lung Adenocarcinoma.
abstract: Guanine (G)-rich oligonucleotides have attracted considerable interest as therapeutic agents. Two G-rich aptamers were selected against epidermal growth factor receptor (EGFR)-transfected A549 cells, and their G-rich domains (S13 and S50) were identified to account for the binding of parental aptamers. Circular dichroism (CD) spectra showed that S13 and S50 bound to their targets by forming parallel quadruplexes. Their binding, internalization, and antiproliferation activity in cancer and noncancer cells were investigated by flow cytometry and 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) assay, and compared with those of nucleolin-binding AS1411 and thrombin-binding aptamer. The two truncated aptamers (S13 and S50) have good binding and internalization in cancer cells and noncancer cells; however, only S50, similar to AS1411, shows potent antiproliferation against cancer cells. Our data suggest that tumor-selective antiproliferation of G-rich oligonucleotides does not directly depend on the binding of the G-rich aptamer to cells.
authors: Molecular Science and Biomedicine Laboratory, State Key Laboratory for Chemo/Bio Sensing and Chemometrics, College of Biology, College of Chemistry and Chemical Engineering, and Collaborative Research Center of Molecular, Engineering for Theranostics, Hunan University, Changsha, 410082, P.R. China.|Hunan Tumor Hospital, Changsha, 410013, P.R. China.
authors: Jun
authors: J
authors: Hu
authors: Molecular Science and Biomedicine Laboratory, State Key Laboratory for Chemo/Bio Sensing and Chemometrics, College of Biology, College of Chemistry and Chemical Engineering, and Collaborative Research Center of Molecular, Engineering for Theranostics, Hunan University, Changsha, 410082, P.R. China.|Center for Research at Bio/Nano Interface, Department of Chemistry and, Department of Physiology and Functional Genomics, Shands Cancer Center, UF Genetics Institute, and McKnight Brain Institute, University of Florida, Gainesville, FL, 32611-7200, USA.
authors: Zilong
authors: Z
authors: Zhao
authors: Molecular Science and Biomedicine Laboratory, State Key Laboratory for Chemo/Bio Sensing and Chemometrics, College of Biology, College of Chemistry and Chemical Engineering, and Collaborative Research Center of Molecular, Engineering for Theranostics, Hunan University, Changsha, 410082, P.R. China.
authors: Qiaoling
authors: Q
authors: Liu
authors: Molecular Science and Biomedicine Laboratory, State Key Laboratory for Chemo/Bio Sensing and Chemometrics, College of Biology, College of Chemistry and Chemical Engineering, and Collaborative Research Center of Molecular, Engineering for Theranostics, Hunan University, Changsha, 410082, P.R. China.
authors: Mao
authors: M
authors: Ye
authors: Hunan Tumor Hospital, Changsha, 410013, P.R. China.
authors: Bingqiang
authors: B
authors: Hu
authors: Hunan Tumor Hospital, Changsha, 410013, P.R. China.
authors: Jing
authors: J
authors: Wang
authors: Molecular Science and Biomedicine Laboratory, State Key Laboratory for Chemo/Bio Sensing and Chemometrics, College of Biology, College of Chemistry and Chemical Engineering, and Collaborative Research Center of Molecular, Engineering for Theranostics, Hunan University, Changsha, 410082, P.R. China. tan@chem.ufl.edu.|Center for Research at Bio/Nano Interface, Department of Chemistry and, Department of Physiology and Functional Genomics, Shands Cancer Center, UF Genetics Institute, and McKnight Brain Institute, University of Florida, Gainesville, FL, 32611-7200, USA. tan@chem.ufl.edu.
authors: Weihong
authors: W
authors: Tan
mesh_terms: D000230:Adenocarcinoma / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D000077192:Adenocarcinoma of Lung; D000970:Antineoplastic Agents / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D052157:Aptamers, Nucleotide / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D001483:Base Sequence; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D066246:ErbB Receptors / Q000037:antagonists & inhibitors* / Q000378:metabolism; D054856:G-Quadruplexes; D006801:Humans; D008168:Lung / Q000187:drug effects / Q000378:metabolism / Q000473:pathology; D008175:Lung Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D008969:Molecular Sequence Data; D009838:Oligodeoxyribonucleotides / Q000494:pharmacology; D010750:Phosphoproteins / Q000378:metabolism; D016601:RNA-Binding Proteins / Q000378:metabolism; D000097796:Nucleolin
chemical_list: D000970:Antineoplastic Agents; D052157:Aptamers, Nucleotide; D066246:ErbB Receptors; D009838:Oligodeoxyribonucleotides; D010750:Phosphoproteins; D016601:RNA-Binding Proteins; D000097796:Nucleolin; C513936:AGRO 100; C081676:thrombin aptamer; C512478:EGFR protein, human
keywords: G-quadruplexes; antiproliferation; aptamers; cancer; cell recognition