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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.

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 Thumbnail


Authors

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BARRIE KELLAM BARRIE.KELLAM@NOTTINGHAM.AC.UK
Professor of Medicinal Chemistry

Carl W. White

Sarah J. Mistry

Mark Soave

Jeanette Woolard

STEPHEN HILL STEVE.HILL@NOTTINGHAM.AC.UK
Professor of Molecular Pharmacology



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

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