TY - JOUR
T1 - Photoswitchable dynasore analogs to control endocytosis with light
AU - Camarero, Núria
AU - Trapero, Ana
AU - Pérez-Jiménez, Ariadna
AU - Macia, Eric
AU - Gomila-Juaneda, Alexandre
AU - Martín-Quirós, Andrés
AU - Nevola, Laura
AU - Llobet, Artur
AU - Llebaria, Amadeu
AU - Hernando, Jordi
AU - Giralt, Ernest
AU - Gorostiza, Pau
N1 - Publisher Copyright:
© The Royal Society of Chemistry.
PY - 2020/9/7
Y1 - 2020/9/7
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=85090027664&partnerID=8YFLogxK
U2 - 10.1039/d0sc03820b
DO - 10.1039/d0sc03820b
M3 - Article
AN - SCOPUS:85090027664
SN - 2041-6520
VL - 11
SP - 8981
EP - 8988
JO - Chemical Science
JF - Chemical Science
IS - 33
ER -