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Campo DC | Valor | Lengua/Idioma |
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dc.contributor.author | Sánchez del Campo Ferrer, Luis | - |
dc.contributor.author | Tárraga Tomás, Alberto | - |
dc.contributor.author | Montenegro Arce, María Fernanda | - |
dc.contributor.author | Cabezas Herrera, Juan | - |
dc.contributor.author | Rodríguez López, José Neptuno | - |
dc.contributor.other | Facultades, Departamentos, Servicios y Escuelas::Departamentos de la UMU::Bioquímica y Biología Molecular A | es |
dc.date.accessioned | 2023-12-22T12:01:50Z | - |
dc.date.available | 2023-12-22T12:01:50Z | - |
dc.date.issued | 2009-04-09 | - |
dc.identifier.citation | Molecular Pharmaceutics. Volumen 6. nº3. Páginas 883-894 | es |
dc.identifier.issn | 1543-8384 | - |
dc.identifier.uri | http://hdl.handle.net/10201/136891 | - |
dc.description | This is an Accepted Manuscript version of the following article, accepted for publication in [Molecular Pharmaceutics]. [Sánchez-del-Campo L, Tárraga A, Montenegro MF, Cabezas-Herrera J, Rodríguez-López JN. Melanoma activation of 3-o-(3,4,5-trimethoxybenzoyl)-(-)-epicatechin to a potent irreversible inhibitor of dihydrofolate reductase. Mol Pharm. 2009 May-Jun;6(3):883-94. doi: 10.1021/mp800259k]. It is deposited under the terms of the Creative Commons Attribution-Non Commercial License (http://creativecommons.org/licenses/by-nc-nd/4.0/), which permits non-commercial reuse, distribution, and reproduction in any medium, provided the original work is properly cited. | es |
dc.description | ©2009. This manuscript version is made available under the CC-BY-NC-ND 4.0 license http://creativecommons.org/licenses/by-nc-nd/4.0/ This document is the Accepted version of a Published Work that appeared in final form in Molecular Pharmaceutics. To access the final edited and published work see https://doi.org/10.1021/mp800259k | es |
dc.description.abstract | Human melanoma is a significant clinical problem because it is resistant to treatment by most chemotherapeutic agents, including antifolates. It is therefore a desirable goal to develop a second generation of low-toxicity antifolate drugs to overcome acquired resistance to the prevention and treatment of this skin pathology. In our efforts to improve the stability and bioavailability of green tea polyphenols for cancer therapy, we synthesized a trimethoxy derivative of epicatechin-3-gallate, which showed high anti proliferative and proapoptotic activity against melanoma. This derivative, 3-O-(3,4,5-trimethoxybenzoyl)-(-)-epicatechin (TMECG), is a prodrug that is selectively activated by the specific melanocyte enzyme tyrosinase. Upon activation, TMECG generates a stable quinone methide product that strongly inhibits dihydrofolate reductase in an irreversible manner. The treatment of melanoma cells with TMECG also affected cellular folate transport and the gene expression of DHFR, which supported the antifolate nature of this compound. In addition, its pharmacological efficacy has been confirmed in a mouse melanoma model, in which tumor growth and metastasis were inhibited, significantly enhancing the mean survival of the treated groups. TMECG, therefore, shows a potential for clinical use in melanoma therapy. | es |
dc.format | application/pdf | es |
dc.format.extent | 37 | es |
dc.language | eng | es |
dc.relation | Ámbito del proyecto: Nacional y regional. Agencia financiadora: Ministerio de Educación y Ciencia y Fundación Séneca (Comunidad Autónoma de Murcia) Código o número del acuerdo de subvención: SAF2006-07040-C02-01, SAF2006-07040-C02-02, 02970/PI/05 | es |
dc.relation.isreplacedby | DOI10.1021/mp800259k | es |
dc.rights | info:eu-repo/semantics/openAccess | es |
dc.rights.uri | http://creativecommons.org/licenses/by-nc-nd/4.0/ | * |
dc.subject | Melanoma | es |
dc.subject | Fólico | es |
dc.subject | Dihydrofolate reductase | es |
dc.subject | Antifolates | es |
dc.subject | Prodrug activation | es |
dc.subject | Ácido | es |
dc.subject.other | CDU::5 - Ciencias puras y naturales::57 - Biología::577 - Bioquímica. Biología molecular. Biofísica | es |
dc.title | Melanoma Activation of 3-O-(3,4,5-Trimethoxybenzoyl)-(-)-Epicatechin to a Potent Irreversible Inhibitor of Dihydrofolate Reductase | es |
dc.type | info:eu-repo/semantics/article | es |
dc.relation.publisherversion | https://doi.org/10.1021/mp800259k | es |
dc.identifier.doi | https://doi.org/10.1021/mp800259k | - |
Aparece en las colecciones: | Artículos: Bioquímica y Biología Molecular "A" |
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Fichero | Descripción | Tamaño | Formato | |
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Mol Pharm Melanoma 2009.pdf | 766,34 kB | Adobe PDF | Visualizar/Abrir |
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