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Título:	A Photoswitchable Antimetabolite for Targeted Photoactivated Chemotherapy
Autor/a:	Matera, Carlo; Gomila Juaneda, Alexandre; Camarero, Núria; Libergoli, Michela; Soler Prat, Concepció; Gorostiza Langa, Pablo Ignacio
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
Materia(s):	-Artritis reumatoide -Psoriasi -Càncer -Fototeràpia -Fotoquimioteràpia -Nanomedicina -Rheumatoid arthritis -Psoriasis -Cancer -Phototherapy -Photochemotherapy -Nanomedicine
Derechos:	(c) American Chemical Society , 2018
Tipo de documento:	Artículo Artículo - Versión aceptada
Editor:	American Chemical Society
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