dc.creator | Gálvez, Marina | es |
dc.creator | Martín Cordero, Carmen | es |
dc.creator | Ayuso, María Jesús | es |
dc.date.accessioned | 2022-04-08T11:24:04Z | |
dc.date.available | 2022-04-08T11:24:04Z | |
dc.date.issued | 2005 | |
dc.identifier.citation | Gálvez, M., Martín Cordero, C. y Ayuso, M.J. (2005). Iridoids as DNA topoisomerase I poisons. Journal of Enzyme Inhibition and Medicinal Chemistry, 20 (4), 389-392. | |
dc.identifier.issn | 1475-6366 | es |
dc.identifier.uri | https://hdl.handle.net/11441/131992 | |
dc.description.abstract | The discovery of new topoisomerase I inhibitors is necessary since most of the antitumor drugs are targeted against type II and
only a very few can specifically affect type I. Topoisomerase poisons generate toxic DNA damage by stabilization of the
covalent DNA-topoisomerase cleavage complex and some have therapeutic efficacy in human cancer. Two iridoids, aucubin
and geniposide, have shown antitumoral activities, but their activity against topoisomerase enzymes has not been tested. Here
it was found that both compounds are able to stabilize covalent attachments of the topoisomerase I subunits to DNA at sites of
DNA strand breaks, generating cleavage complexes intermediates so being active as poisons of topoisomerase I, but not
topoisomerase II. This result points to DNA damage induced by topoisomerase I poisoning as one of the possible mechanisms
by which these two iridoids have shown antitumoral activity, increasing interest in their possible use in cancer
chemoprevention and therapy. | es |
dc.description.sponsorship | Ministerio de Ciencia y Tecnología de España. SAF 2000-0167 | es |
dc.format | application/pdf | es |
dc.format.extent | 4 p. | es |
dc.language.iso | eng | es |
dc.publisher | Taylor & Francis Open Access | es |
dc.relation.ispartof | Journal of Enzyme Inhibition and Medicinal Chemistry, 20 (4), 389-392. | |
dc.rights | Attribution-NonCommercial-NoDerivatives 4.0 Internacional | * |
dc.rights.uri | http://creativecommons.org/licenses/by-nc-nd/4.0/ | * |
dc.subject | Aucubin | es |
dc.subject | geniposide | es |
dc.subject | iridoids | es |
dc.subject | topoisomerase I | es |
dc.subject | poison | es |
dc.subject | inhibition | es |
dc.title | Iridoids as DNA topoisomerase I poisons | es |
dc.type | info:eu-repo/semantics/article | es |
dcterms.identifier | https://ror.org/03yxnpp24 | |
dc.type.version | info:eu-repo/semantics/publishedVersion | es |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | es |
dc.contributor.affiliation | Universidad de Sevilla. Departamento de Farmacología | es |
dc.relation.projectID | SAF 2000-0167 | es |
dc.relation.publisherversion | https://doi.org/10.1080/14756360500141879 | es |
dc.identifier.doi | 10.1080/14756360500141879 | es |
dc.journaltitle | Journal of Enzyme Inhibition and Medicinal Chemistry | es |
dc.publication.volumen | 20 | es |
dc.publication.issue | 4 | es |
dc.publication.initialPage | 389 | es |
dc.publication.endPage | 392 | es |
dc.identifier.sisius | 6609352 | es |
dc.contributor.funder | Ministerio de Ciencia y Tecnología (MCYT). España | es |