2021 Volume 61 Issue 6 Pages 366-369
G protein-coupled receptors (GPCRs) constitute one of the largest superfamily of proteins in the human genome. Since GPCRs are major drug targets, a pharmacological evaluation of compounds on a GPCR is an important process in drug discovery. Here, we review the past trends of the in cell single-molecule measurement of GPCRs, many of which were focused on dimerization of GPCRs. Then, we introduce our recent study regarding the drug evaluation based on a general feature of a diffusion-function relationship of GPCRs. We also discuss the future applicability of the present study in pharmacology and drug screening.
