Application of Quantitative Fluorescence Microscopic Approaches to Monitor Organization and Dynamics of the Serotonin1A Receptor

Abstract

G protein-coupled receptors (GPCRs) are the largest class of molecules involved in signal transduction across membranes and represent major targets in the development of novel drug candidates in all clinical areas. Recent advances in understanding of the nonrandom distribution of GPCRs, G proteins, and effector molecules have given rise to new challenges and complexities in cellular signaling by GPCRs. In this article, we provide specific examples on the application of quantitative fluorescence microscopic approaches to monitor organization and dynamics of the serotonin 1A receptor (a GPCR) in live cells. This assumes broader relevance due to the emerging theme that GPCR function depends on its organi-zation and dynamics. We envisage that with progress in understanding of receptor organization and dynamics, our knowledge of GPCR function would improve considerably, thereby enabling to design better therapeutic strategies to combat diseases related to malfunctioning of GPCRs.