Visualization of membrane localization and the functional state of CB₂R pools using matched agonist and inverse agonist probe pairs.

ABSTRACT: The diversity of physiological roles of the endocannabinoid system has turned it into an attractive yet elusive therapeutic target. However, chemical probes with various functionalities could pave the way for a better understanding of the endocannabinoid system at the cellular level. Notably, inverse agonists of CB₂R - a key receptor of the endocannabinoid system - lagged behind despite the evidence regarding the therapeutic potential of its antagonism. Herein, we report a matched fluorescent probe pair based on a common chemotype to address and visualize both the active and inactive states of CB₂R, selectively. Alongside extensive cross-validation by flow cytometry, time-lapse confocal microscopy, and super-resolution microscopy, we successfully visualize the intrace

SUBMITTER: Wasinska-Kalwa M 

PROVIDER: S-EPMC11485011 | biostudies-literature | 2024 Oct

REPOSITORIES: biostudies-literature