Activation of P2X4 receptors induces an increase in the area of the extracellular region and a decrease in receptor mobility

Bergler, Frederik; Fuentes, Christian; Kadir, Md. Fahim; Navarrete, Camilo; Supple, Jack; Barrera, Nelson P.; Edwardson, John Michael


The P2X4 receptor (P2X4R) is an ATP-gated cation channel. Here, we used fast-scan atomic force microscopy (AFM) to visualize changes in the structure and mobility of individual P2X4Rs in response to activation. P2X4Rs were purified from detergent extracts of transfected cells and integrated into lipid bilayers. Activation resulted in a rapid (2 s) and substantial (10-20 nm(2)) increase in the cross-sectional area of the extracellular region of the receptor and a corresponding decrease in receptor mobility. Both effects were blocked by the P2X4R antagonist 5-BDBD. Addition of cholesterol to the bilayer reduced receptor mobility, although the ATP-induced reduction in mobility was still observed. We suggest that the observed responses to activation may have functional consequences for purinergic signalling.

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Título según WOS: ID WOS:000577977400001 Not found in local WOS DB
Título de la Revista: FEBS LETTERS
Volumen: 594
Número: 24
Fecha de publicación: 2020
Página de inicio: 4381
Página final: 4389


Notas: ISI