Photoswitchable dynasore analogs to control endocytosis with light

Núria Camarero, Ana Trapero, Ariadna Pérez-Jiménez, Eric Macia, Alexandre Gomila-Juaneda, Andrés Martín-Quirós, Laura Nevola, Artur Llobet, Amadeu Llebaria, Jordi Hernando, Ernest Giralt, Pau Gorostiza*

*Corresponding author for this work

Research output: Contribution to journalArticleResearchpeer-review

4 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)8981-8988
Number of pages8
JournalChemical Science
Volume11
Issue number33
DOIs
Publication statusPublished - 7 Sept 2020

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