Modulation of P2X₇ receptor functions by polymyxin B: crucial role of the hydrophobic tail of the antibiotic molecule

Abstract

The effects of polymyxin B depended on the presence of its N-terminal fatty amino acid 6-methylheptanoic/octanoic-Dab residue as deletion of this residue abolished polymyxin B-dependent modulation of ATP-triggered responses. These findings are important in the search for allosteric modulators of the P2X7 receptor.