Data di Pubblicazione:
2018
Citazione:
A photoswitchable antimetabolite for targeted photoactivated chemotherapy / C. Matera, A. Gomila-Juaneda, N. Camarero, M. Libergoli, C. Soler, P. Gorostiza. ((Intervento presentato al 2. convegno International Symposium on Photopharmacology (ISPP) tenutosi a Vic, Barcelona nel 2018.
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 analog 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.[1]
Reference
1. Matera, C.; Gomila-Juaneda, A.; Camarero, N.; Libergoli, M.; Soler, C.; Gorostiza, P. J. Am. Chem. Soc., DOI: 10.1021/jacs.8b08249.
Tipologia IRIS:
14 - Intervento a convegno non pubblicato
Elenco autori:
C. Matera, A. Gomila-Juaneda, N. Camarero, M. Libergoli, C. Soler, P. Gorostiza
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