How structure informs and transforms chemogenetics

Chemogenetic technologies such as Designer Receptors Exclusively Activated by Designer Drugs (DREADDs) are widely used to remotely control neuronal and non-neuronal signaling. DREADDs exist for most of the canonical G protein-coupled receptor signaling pathways, and provide a synthetic biology platform useful for elucidating the role of neuronal signaling for brain function. Here, a focused review is provided that shows how recent insights obtained from GPCR structural studies inform our understanding of these chemogenetic tools from a structural perspective.