Host: The Japanese Pharmacological Society
Name : The 95th Annual Meeting of the Japanese Pharmacological Society
Number : 95
Location : Fukuoka
Date : March 07, 2022 - March 09, 2022
Membrane receptors including G protein-coupled receptors (GPCRs), receptor tyrosine kinases (RTKs) and ion channels are major drug targets. We have demonstrated that GPCR molecules generally accumulate into membrane domains upon activation. Here we show that the signaling bias of an angiotensin receptor (AT1R) is regulated by the membrane domain colocalization of receptor/G protein/GRK using multicolor single-molecule imaging. We also show that the different kinetics of endocytosis between TRPV1 and TRPV4 channels are derived from the pre-accumulation of TRPV channels in membrane domains before activation by single-molecule time-lapse imaging. Single-molecule imaging provides us a lot of information including protein-protein interaction, diffusion dynamics, and oligomerization of proteins in living cells, which cannot be obtained by a conventional high content analyzer. In order to utilize the single-molecule imaging to pharmacology, we are currently developing a multicolor single-molecule imaging system that enables us to monitor cells in a 96-well plate automatically. We will discuss the future development of the next generation high content analyzer based on single molecule imaging.
