Identification of residues involved in homotrimeric assembly of the human P2X4 receptor by simulations and site-directed mutagenesis.

Abstract

P2X receptors (P2XRs) are a family of ATP-gated cation channels with seven members, P2X1-P2X7. P2XRs are involved in numerous physiological and pathophysiological functions and are therefore interesting drug targets. Functional P2XRs are obligate homotrimers or heterotrimers of three identical or homologous subunits, respectively, with each subunit having a large ectodomain flanked by two membrane-spanning helices, TM1 and TM2, and N- and C-terminal intracellular domains.