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http://hdl.handle.net/2445/126377
Title: | A Photoswitchable Antimetabolite for Targeted Photoactivated Chemotherapy |
Author: | Matera, Carlo Gomila Juaneda, Alexandre Camarero, Núria Libergoli, Michela Soler Prat, Concepció Gorostiza Langa, Pablo Ignacio |
Keywords: | Artritis reumatoide Psoriasi Càncer Fototeràpia Fotoquimioteràpia Nanomedicina Rheumatoid arthritis Psoriasis Cancer Phototherapy Photochemotherapy Nanomedicine |
Issue Date: | 10-Oct-2018 |
Publisher: | American Chemical Society |
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 |
Note: | Versió postprint del document publicat a: https://doi.org/10.1021/jacs.8b08249 |
It is part of: | Journal of the American Chemical Society, 2018, vol. 140 , num. 46, p. 15764-15773 |
URI: | http://hdl.handle.net/2445/126377 |
Related resource: | https://doi.org/10.1021/jacs.8b08249 |
ISSN: | 0002-7863 |
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)) |
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