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. 2019 Apr 9;13:121. doi: 10.3389/fncel.2019.00121

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Copyright © 2019 Ase, Therrien and Séguéla.

This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.

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A single residue in the ectodomain, Ile312 in human P2X4, determines BX430 antagonist effect and sensitivity of P2X4 orthologs. (A) Alignment of a subregion of the ectodomain of human P2X4 with several vertebrate P2X4 orthologs showing Ile312 in its proximal environment. r, rat; m, mouse; b, bovine; x, xenopus; zf, zebrafish. (B,C) Representative traces and quantitative results showing a complete loss of sensitivity to BX430 caused by the single mutation I312T on human P2X4 receptor channels expressed in HEK293 cells. (D,E) Representative traces and quantitative results showing the gain of sensitivity to BX430 caused by the single mutation T312I on rat P2X4 receptor channels. ***P < 0.001 (n = 5–8).