Engineered Chemogenetically-Gated Ion Channel

Engineered chemogenetically-gated ion channels are genetically modified ion channels that can be selectively activated or inhibited by otherwise inert, exogenous small molecules (ligands). These tools allow precise, reversible, and noninvasive control of cellular excitability in specific cell populations—most commonly neurons. Activation leads to ion flow across the membrane altering cell excitability, and the effect can be excitatory or inhibitory depending on the design. Compared to optogenetics, chemogenetic systems offer less invasiveness but slower kinetics.

Other names

Chemogenetically-gated ion channelPSAM/PSEM SystemPharmacologically Selective Actuator ModulesEngineered LGICs

Activation or inhibition of engineered ion channels by exogenous, inert small molecule ligands (PSEMs), leading to altered cellular excitability via ion flux. The channel is expressed in target cells using genetic methods; activated/inhibited upon administration of a specific exogenous small-molecule agonist/antagonist that does not affect native receptors.