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

Kellam, Barrie; White, Carl W.; Goulding, Joëlle; Mistry, Sarah J.; Soave, Mark; Woolard, Jeanette; Briddon, Stephen J.; Hill, Stephen J.

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 (β2AR) antagonist ICI 118,551. The majority of fluorescent ICI 118,551 analogs had good affinity for the β2AR (pKD >7.0) with good selectivity over the β1AR (pKD

• Journal Article Type: Article
• Acceptance Date: Mar 31, 2021
• Online Publication Date: May 18, 2021
• Publication Date: Jun 1, 2021
• Deposit Date: Apr 12, 2021
• Publicly Available Date: May 18, 2021
• Journal: Pharmacology Research & Perspectives
• Electronic ISSN: 2052-1707
• Peer Reviewed: Peer Reviewed
• Volume: 9
• Issue: 3
• Article Number: e00779
• DOI: https://doi.org/10.1002/prp2.779
• Keywords: ICI 118; 551; fluorescent ligands; NanoBRET; CRISPR/Cas9 genome editing; ligand-binding; β2-adrenoceptors
• Public URL: https://nottingham-repository.worktribe.com/output/5461017
• Publisher URL: https://bpspubs.onlinelibrary.wiley.com/doi/10.1002/prp2.779