Gel-Free Tools for Quick and Simple Screening of Anti-Topoisomerase 1 Compounds
dc.contributor.author | Keller, Josephine Geertsen | |
dc.contributor.author | Petersen, Kamilla Vandsø | |
dc.contributor.author | Mizielinski, Karol | |
dc.contributor.author | Thiesen, Celine | |
dc.contributor.author | Bjergbæk, Lotte | |
dc.contributor.author | Reguera, Rosa M. | |
dc.contributor.author | Pérez-Pertejo, Yolanda | |
dc.contributor.author | Balaña-Fouce, Rafael | |
dc.contributor.author | Trejo, Ángela | |
dc.contributor.author | Masdeu Margalef, Carme | |
dc.contributor.author | Alonso Pérez, Concepción Estibaliz | |
dc.contributor.author | Knudsen, Birgitta R. | |
dc.contributor.author | Tesauro, Cinzia | |
dc.date.accessioned | 2023-06-08T16:09:49Z | |
dc.date.available | 2023-06-08T16:09:49Z | |
dc.date.issued | 2023-04-27 | |
dc.identifier.citation | Pharmaceuticals 16(5) : (2023) // Article ID 657 | es_ES |
dc.identifier.issn | 1424-8247 | |
dc.identifier.uri | http://hdl.handle.net/10810/61332 | |
dc.description.abstract | With the increasing need for effective compounds against cancer or pathogen-borne diseases, the development of new tools to investigate the enzymatic activity of biomarkers is necessary. Among these biomarkers are DNA topoisomerases, which are key enzymes that modify DNA and regulate DNA topology during cellular processes. Over the years, libraries of natural and synthetic small-molecule compounds have been extensively investigated as potential anti-cancer, anti-bacterial, or anti-parasitic drugs targeting topoisomerases. However, the current tools for measuring the potential inhibition of topoisomerase activity are time consuming and not easily adaptable outside specialized laboratories. Here, we present rolling circle amplification-based methods that provide fast and easy readouts for screening of compounds against type 1 topoisomerases. Specific assays for the investigation of the potential inhibition of eukaryotic, viral, or bacterial type 1 topoisomerase activity were developed, using human topoisomerase 1, Leishmania donovani topoisomerase 1, monkeypox virus topoisomerase 1, and Mycobacterium smegmatis topoisomerase 1 as model enzymes. The presented tools proved to be sensitive and directly quantitative, paving the way for new diagnostic and drug screening protocols in research and clinical settings. | es_ES |
dc.description.sponsorship | This research was funded in part by the Ministerio de Ciencia e Innovación, Spain (PID2021-122558OB-I00, UE) and by Gobierno Vasco, Universidad del País Vasco (GV, IT1701-22; UPV). | es_ES |
dc.language.iso | eng | es_ES |
dc.publisher | MDPI | es_ES |
dc.relation | info:eu-repo/grantAgreement/MCIN/PID2021-122558OB-I00 | es_ES |
dc.rights | info:eu-repo/semantics/openAccess | es_ES |
dc.rights.uri | http://creativecommons.org/licenses/by-nc-nd/4.0/ | |
dc.subject | human topoisomerase 1 | es_ES |
dc.subject | Mycobacterium smegmatis topoisomerase 1 | es_ES |
dc.subject | Leishmania donovani topoisomerase 1 | es_ES |
dc.subject | monkeypox virus topoisomerase 1 | es_ES |
dc.subject | enzyme activity | es_ES |
dc.subject | rolling circle amplification | es_ES |
dc.subject | drug screening | es_ES |
dc.title | Gel-Free Tools for Quick and Simple Screening of Anti-Topoisomerase 1 Compounds | es_ES |
dc.type | info:eu-repo/semantics/article | es_ES |
dc.date.updated | 2023-05-26T13:20:52Z | |
dc.rights.holder | © 2023 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). | es_ES |
dc.relation.publisherversion | https://www.mdpi.com/1424-8247/16/5/657 | es_ES |
dc.identifier.doi | 10.3390/ph16050657 | |
dc.departamentoes | Química orgánica I | |
dc.departamentoeu | Kimika organikoa I |
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Except where otherwise noted, this item's license is described as © 2023 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).