Synthesis and Characterization of Photoswitchable Covalent Ligands for the β₂-Adrenoceptor.

ABSTRACT: The β₂-adrenergic receptor (β₂AR) is a critical target for the treatment of airway diseases such as asthma or chronic obstructive pulmonary disease (COPD). To better understand its mechanism of action and study its dynamics, photoswitchable ligands provide a distinct advantage due to their ability to be activated with high spatiotemporal control. In this study, we developed a series of molecular tools featuring different combinations of pharmacophores, covalent warheads, and linker lengths. These compounds were characterized using highly specific assay protocols to evaluate their covalent binding capabilities, with the goal of identifying optimal covalently-bound photoswitches. Among these, the covalently-bound photoswitchable receptor agonist 6 exhibited a significan

SUBMITTER: Wirth U 

PROVIDER: S-EPMC12144893 | biostudies-literature | 2025 Jun

REPOSITORIES: biostudies-literature