Abstract: | The use of nanoparticle (NP) systems to control cellular physiology, including membrane potential, can facilitate furthered understanding of many disparate cellular processes ranging from cellular proliferation to tissue regeneration. A gold NP (AuNP) bioconjugate system based on the honeybee venom peptide, tertiapin‐Q (AuNP‐TPN‐Q), that depolarizes membrane potential by targeting inward rectifier potassium channels (Kir), is developed. The conjugate elicits, in a peptide concentration–dependent manner, a greater and more rapid depolarization response compared to the free peptide alone. The specificity of the interaction of the AuNP‐TPN‐Q conjugate with the Kir channel using immunocytochemistry and competition binding assays is confirmed. It is further shown that membrane depolarization is photothermally reversible via the laser‐induced plasmonic heating of the AuNP, providing a level of control over Kir channels not afforded by currently available drugs. The functional nanobioconjugate described herein provides a new research tool for understanding the intricacies of ion channel activity and the modulation of cellular membrane potential. |