1. Chemogenetic Receptors
There are many chemogenetic platforms based on GPCRs modification,
such as allele-specific activation of genetically encoded receptors,
receptors activated solely by synthetic ligands (RASSLs), genetically
engineered receptors, and designer receptors exclusively activated by
designer drugs (DREADDs). Among them, DREADDs have become the
most widely used chemical genetics technology. There are many
DREADDs activated by azizapine-N-oxide. They will selectively act on
different GPCR signaling cascades, including activation of Gq, Gi, Gs, Golf,
and β-arrestin. The most widely used DREADDs are Gq-DREADD and Gi-
DREADD.
Fig.6 Evolutionary timeline of GPCR-based chemogenetic approaches listing the main
corresponding tools starting with allele-specific engineered β-adrenergic receptors,
RASSLs, and DREADDs.
Chemogenetics
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