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Activation of P2X4 receptors induces an increase in the area of the extracellular region and a decrease in receptor mobility
Author(s) -
Bergler Frederik,
Fuentes Christian,
Kadir Md. Fahim,
Navarrete Camilo,
Supple Jack,
Barrera Nelson P.,
Edwardson John Michael
Publication year - 2020
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1002/1873-3468.13942
Subject(s) - purinergic receptor , extracellular , receptor , chemistry , biophysics , p2 receptor , hek 293 cells , microbiology and biotechnology , biochemistry , biology
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.