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

Citation

Kellam, B., White, C. W., Goulding, J., Mistry, S. J., Soave, M., Woolard, J., …Hill, S. J. (2021). 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. Pharmacology Research and Perspectives, 9(3), Article e00779. https://doi.org/10.1002/prp2.779

• 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
• Publisher: Wiley Open Access
• 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