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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
Rheumatoid arthritis
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:
It is part of: Journal of the American Chemical Society, 2018, vol. 140 , num. 46, p. 15764-15773
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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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