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Photoswitchable dynasore analogs to control endocytosis with light

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The spatiotemporal control of cellular dynamic processes has great fundamental interest but lacks versatile molecular tools. Dynamin is a key protein in endocytosis and an appealing target to manipulate cell trafficking using patterns of light. We have developed the first photoswitchable small-molecule inhibitors of endocytosis (dynazos), by a stepwise design of the photochromic and pharmacological properties of dynasore, a dynamin inhibitor. We have characterized their photochromism with UV-visible and transient absorption spectroscopy and their biological activity using fluorescence microscopies and flow cytometry. Dynazos are water-soluble, cell permeable, and photostable, and enable fast, single- wavelength photoswitchable inhibition of clathrin-mediated endocytosis at micromolar concentration.

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CAMARERO, Núria, TRAPERO, Ana, PÉREZ JIMÉNEZ, Ariadna, MACIA, Eric, GOMILA JUANEDA, Alexandre, GOROSTIZA LANGA, Pablo ignacio, NEVOLA, Laura, LLOBET BERENGUER, Artur, LLEBARIA SOLDEVILA, Amadeu, HERNANDO, Jordi, GIRALT LLEDÓ, Ernest. Photoswitchable dynasore analogs to control endocytosis with light. _Chemical Science_. 2020. Vol. 11, núm. 8981-8988. [consulta: 29 de gener de 2026]. ISSN: 2041-6520. [Disponible a: https://hdl.handle.net/2445/173364]

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