Please use this identifier to cite or link to this item:
http://hdl.handle.net/2445/126377
Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | Matera, Carlo | - |
dc.contributor.author | Gomila Juaneda, Alexandre | - |
dc.contributor.author | Camarero, Núria | - |
dc.contributor.author | Libergoli, Michela | - |
dc.contributor.author | Soler Prat, Concepció | - |
dc.contributor.author | Gorostiza Langa, Pablo Ignacio | - |
dc.date.accessioned | 2018-11-23T10:52:22Z | - |
dc.date.available | 2019-10-10T05:10:17Z | - |
dc.date.issued | 2018-10-10 | - |
dc.identifier.issn | 0002-7863 | - |
dc.identifier.uri | http://hdl.handle.net/2445/126377 | - |
dc.description.abstract | The efficacy and tolerability of systemically administered anticancer agents are limited by their off-target effects. Precise spatiotemporal control over their cytotoxic activity would allow improving chemotherapy treatments, and light-regulated drugs are well suited to this purpose. We have developed phototrexate, the first photoswitchable inhibitor of the human dihydrofolate reductase (DHFR), as a photochromic analogue of methotrexate, a widely prescribed chemotherapeutic drug to treat cancer and psoriasis. Quantification of the light-regulated DHFR enzymatic activity, cell proliferation, and in vivo effects in zebrafish show that phototrexate behaves as a potent antifolate in its photoactivated cis configuration and that it is nearly inactive in its dark-relaxed trans form. Thus, phototrexate constitutes a proof-of-concept to design light-regulated cytotoxic small molecules and a step forward to develop targeted anticancer photochemotherapies with localized efficacy and reduced adverse effects | - |
dc.format.extent | 10 p. | - |
dc.format.mimetype | application/pdf | - |
dc.language.iso | eng | - |
dc.publisher | American Chemical Society | - |
dc.relation.isformatof | Versió postprint del document publicat a: https://doi.org/10.1021/jacs.8b08249 | - |
dc.relation.ispartof | Journal of the American Chemical Society, 2018, vol. 140 , num. 46, p. 15764-15773 | - |
dc.relation.uri | https://doi.org/10.1021/jacs.8b08249 | - |
dc.rights | (c) American Chemical Society , 2018 | - |
dc.source | Articles publicats en revistes (Patologia i Terapèutica Experimental) | - |
dc.subject.classification | Artritis reumatoide | - |
dc.subject.classification | Psoriasi | - |
dc.subject.classification | Càncer | - |
dc.subject.classification | Fototeràpia | - |
dc.subject.classification | Fotoquimioteràpia | - |
dc.subject.classification | Nanomedicina | - |
dc.subject.other | Rheumatoid arthritis | - |
dc.subject.other | Psoriasis | - |
dc.subject.other | Cancer | - |
dc.subject.other | Phototherapy | - |
dc.subject.other | Photochemotherapy | - |
dc.subject.other | Nanomedicine | - |
dc.title | A Photoswitchable Antimetabolite for Targeted Photoactivated Chemotherapy | - |
dc.type | info:eu-repo/semantics/article | - |
dc.type | info:eu-repo/semantics/acceptedVersion | - |
dc.identifier.idgrec | 682930 | - |
dc.date.updated | 2018-11-23T10:52:23Z | - |
dc.relation.projectID | info:eu-repo/grantAgreement/EC/H2020/785907/EU//HBP SGA2 | - |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | - |
dc.identifier.pmid | 30346152 | - |
Appears in Collections: | Articles publicats en revistes (Patologia i Terapèutica Experimental) Articles publicats en revistes (Institut d'lnvestigació Biomèdica de Bellvitge (IDIBELL)) Articles publicats en revistes (Institut de Bioenginyeria de Catalunya (IBEC)) |
Files in This Item:
File | Description | Size | Format | |
---|---|---|---|---|
682930.pdf | 12.66 MB | Adobe PDF | View/Open |
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.