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Article

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Accepted version

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2018-10-10

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Please use this identifier to cite or link to this item: https://hdl.handle.net/2445/126377

A Photoswitchable Antimetabolite for Targeted Photoactivated Chemotherapy

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https://doi.org/10.1021/jacs.8b08249

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

Subject

Artritis reumatoide, Psoriasi, Càncer, Fototeràpia, Fotoquimioteràpia, Nanomedicina

Subject (English)

Rheumatoid arthritis, Psoriasis, Cancer, Phototherapy, Photochemotherapy, Nanomedicine

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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))

Citation

MATERA, Carlo, et al. A Photoswitchable Antimetabolite for Targeted Photoactivated Chemotherapy. Journal of the American Chemical Society. 2018. Vol. 140, num. 46, pags. 15764-15773. ISSN 0002-7863. [consulted: 11 of August of 2026]. Available at: https://hdl.handle.net/2445/126377

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