Subtype selective fluorescent ligands based on ICI 118,551 to study the human β2-adrenoceptor in CRISPR/Cas9 genome-edited HEK293T cells at low expression levels.

ABSTRACT: Fluorescent ligand technologies have proved to be powerful tools to improve our understanding of ligand-receptor interactions. Here we have characterized a small focused library of nine fluorescent ligands based on the highly selective β₂ -adrenoceptor (β₂ AR) antagonist ICI 118,551. The majority of fluorescent ICI 118,551 analogs had good affinity for the β₂ AR (pK_D >7.0) with good selectivity over the β₁ AR (pK_D <6.0). The most potent and selective ligands being 8c (ICI 118,551-Gly-Ala-BODIPY-FL-X; β₂ AR pK_D 7.48), 9c (ICI 118,551-βAla-βAla-BODIPY-FL-X; β₂ AR pK_D 7.48), 12a (ICI 118,551-PEG-BODIPY-X-630/650; β₂ AR pK_D 7.56), and 12b (ICI 118,551-PEG-BODIPY-F

SUBMITTER: Goulding J 

PROVIDER: S-EPMC8130569 | biostudies-literature | 2021 May

REPOSITORIES: biostudies-literature