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A Photoswitchable Antimetabolite for Targeted Photoactivated Chemotherapy
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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
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MATERA, Carlo, et al. A Photoswitchable Antimetabolite for Targeted Photoactivated Chemotherapy. Journal of the American Chemical Society. 2018. Vol. 140, núm. 46, pàgs. 15764-15773. ISSN 0002-7863. [consulta: 10 de maig de 2026]. Disponible a: https://hdl.handle.net/2445/126377