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Herein, we have studied AS1411 as a supramolecular carrier for the delivery of an acridine-based G-quadruplex ligand, C<jats:sub>8<\/jats:sub>, to HeLa cancer cells. Two AS1411 derivatives, LNA-AS1411 and U-AS1411, were also tested, in an attempt to compare AS1411 pharmacological properties. The results showed that AS1411-C<jats:sub>8<\/jats:sub> complexation was made with great binding strength and that it lowered the ligand\u2019s cytotoxicity towards non-malignant cells. This effect was suggested to be due to a decreased internalization of the complexed versus free C<jats:sub>8<\/jats:sub> as shown by flow cytometry. The AS1411 derivatives, despite forming a stable complex with C<jats:sub>8<\/jats:sub>, lacked the necessary tumour-selective behaviour. The binding of C<jats:sub>8<\/jats:sub> to AS1411 G-quadruplex structure did not negatively affect the recognition of nucleolin by the aptamer. The AS1411-C<jats:sub>8<\/jats:sub> repressed c-MYC expression at the transcriptional level, possibly due to C<jats:sub>8<\/jats:sub> ability to stabilize the c-MYC promoter G-quadruplexes. Overall, this study demonstrates the usefulness of AS1411 as a supramolecular carrier of the G-quadruplex binder C<jats:sub>8<\/jats:sub> and the potential of using its tumour-selective properties for the delivery of ligands for cancer therapy.<\/jats:p>","DOI":"10.1038\/s41598-019-44388-9","type":"journal-article","created":{"date-parts":[[2019,5,28]],"date-time":"2019-05-28T10:03:45Z","timestamp":1559037825000},"update-policy":"https:\/\/doi.org\/10.1007\/springer_crossmark_policy","source":"Crossref","is-referenced-by-count":107,"title":["Aptamer-based Targeted Delivery of a G-quadruplex Ligand in Cervical Cancer Cells"],"prefix":"10.1038","volume":"9","author":[{"ORCID":"https:\/\/orcid.org\/0000-0003-3035-4881","authenticated-orcid":false,"given":"Josu\u00e9","family":"Carvalho","sequence":"first","affiliation":[]},{"given":"Artur","family":"Paiva","sequence":"additional","affiliation":[]},{"given":"Maria Paula","family":"Cabral Campello","sequence":"additional","affiliation":[]},{"ORCID":"https:\/\/orcid.org\/0000-0002-9164-0913","authenticated-orcid":false,"given":"Ant\u00f3nio","family":"Paulo","sequence":"additional","affiliation":[]},{"ORCID":"https:\/\/orcid.org\/0000-0003-3043-8401","authenticated-orcid":false,"given":"Jean-Louis","family":"Mergny","sequence":"additional","affiliation":[]},{"ORCID":"https:\/\/orcid.org\/0000-0002-0296-5979","authenticated-orcid":false,"given":"Gilmar F.","family":"Salgado","sequence":"additional","affiliation":[]},{"given":"Jo\u00e3o A.","family":"Queiroz","sequence":"additional","affiliation":[]},{"given":"Carla","family":"Cruz","sequence":"additional","affiliation":[]}],"member":"297","published-online":{"date-parts":[[2019,5,28]]},"reference":[{"key":"44388_CR1","doi-asserted-by":"publisher","first-page":"151","DOI":"10.1016\/j.yexmp.2009.01.004","volume":"86","author":"PJ Bates","year":"2009","unstructured":"Bates, P. 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