2026-04-17T12:23:09Zhttps://riubu.ubu.es/oai/request

oai:riubu.ubu.es:10259/86082024-02-08T01:05:28Zcom_10259_3592com_10259_3591com_10259.4_106com_10259_2604com_10259_3924com_10259_5086col_10259_3930col_10259_3925

Alonso Carrillo, Daniel 761 600 0000-0002-6132-8953 Arias Betancur, Alain 38bb623a-30d8-4c4a-b321-e3d4e5365ce6 600 Carreira Barral, Israel 763 600 0000-0002-4835-8752 Fontova Pale, Pere 766 600 0000-0002-1352-3084 Soto Cerrato, Vanessa 346bb3c7-0c69-4d62-9045-26b0b8d37a51 600 García Valverde, María 222 600 0000-0002-3990-8388 Pérez Tomás, Ricardo 3306d7a2-706a-47ab-8490-869a1b191c58 600 Quesada Pato, Roberto 458 600 0000-0003-2764-7157 2024-02-07T07:45:24Z 2024-02-07T07:45:24Z 2023-09 2589-0042 http://hdl.handle.net/10259/8608 10.1016/j.isci.2023.107898 An excessive production of lactate by cancer cells fosters tumor growth and metastasis. Therefore, targeting lactate metabolism and transport offers a new therapeutic strategy against cancer, based on dependency of some cancer cells for lactate as energy fuel or as oncogenic signal. Herein we present a family of anionophores based on the structure of click-tambjamines that have proved to be extremely active lactate carriers across phospholipid membranes. Compound 1, the most potent lactate transmembrane carrier, was studied in HeLa cells. The use of a monocarboxylate transporters (MCTs) inhibitor proved that 1 is an active lactate transporter in living cells, confirming the results obtained in phospholipid vesicles. Moreover, an additive effect of compound 1 with cisplatin was observed in HeLa cells. Identification of active lactate anionophores working in living cells opens up ways to exploit this class of compounds as molecular tools and drugs addressing dysregulated lactate metabolism. This research has been financially supported by Consejería de Educación de la Junta de Castilla y León (project BU067P20) and Ministerio de Ciencia e Innovación (project PID2020-117610RB-I00). D.A.-C., I.C.-B. and P.F. thank Consejería de Educación de la Junta de Castilla y León, European Regional Development Fund (ERDF) and European Social Fund (ESF) for their pre-doctoral (D.A.-C.) and post-doctoral (I.C.-B. and P.F.) contracts. A.A.-B. thanks to PFCHA/Becas Chile (Folio#72200156). The authors gratefully acknowledge Andrea Sancho-Medina for her contributions to transmembrane anion transport experiments. application/pdf eng Elsevier iScience. 2023, V. 26, n. 10, 107898 https://doi.org/10.1016/j.isci.2023.107898 Attribution-NonCommercial-NoDerivatives 4.0 Internacional http://creativecommons.org/licenses/by-nc-nd/4.0/ info:eu-repo/semantics/openAccess Biología molecular Química orgánica Bioquímica Molecular biology Chemistry, Organic Biochemistry Small molecule anion carriers facilitate lactate transport in model liposomes and cells info:eu-repo/semantics/article info:eu-repo/semantics/publishedVersion iScience 26 10 THUMBNAIL Alonso-iScience_2023.pdf.jpg Alonso-iScience_2023.pdf.jpg IM Thumbnail image/jpeg 3323 https://riubu.ubu.es/bitstream/10259/8608/4/Alonso-iScience_2023.pdf.jpg 4e40d6891adea88311892645647df317 MD5 4 LICENSE license.txt license.txt text/plain; charset=utf-8 999 https://riubu.ubu.es/bitstream/10259/8608/3/license.txt b295bcbce42e2caabeb0c623d3860c06 MD5 3 CC-LICENSE license_rdf license_rdf application/rdf+xml; charset=utf-8 805 https://riubu.ubu.es/bitstream/10259/8608/2/license_rdf 4460e5956bc1d1639be9ae6146a50347 MD5 2 ORIGINAL Alonso-iScience_2023.pdf Alonso-iScience_2023.pdf application/pdf 4166314 https://riubu.ubu.es/bitstream/10259/8608/1/Alonso-iScience_2023.pdf a1e88942e94f75b84ffa3e8cd9d34d28 MD5 1 10259/8608 oai:riubu.ubu.es:10259/8608 2024-02-08 02:05:28.969 Repositorio Institucional de la Universidad de Burgos bubrep@ubu.es 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