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.

Adrenergic beta-2 Receptor Antagonists / pharmacology CRISPR-Cas Systems Fluorescence Gene Editing HEK293 Cells Humans Ligands Propanolamines / pharmacology Receptors, Adrenergic, beta-2 / genetics
CRISPR/Cas9 genome editing ICI 118,551 NanoBRET fluorescent ligands ligand binding β2-adrenoceptors

Journal

Pharmacology research & perspectives
ISSN: 2052-1707
Titre abrégé: Pharmacol Res Perspect
Pays: United States
ID NLM: 101626369

Informations de publication

Date de publication:
05 2021
Historique:
revised: 30 03 2021
received: 23 01 2021
accepted: 31 03 2021
entrez: 18 5 2021
pubmed: 19 5 2021
medline: 1 2 2022
Statut: ppublish

Résumé

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 β

Identifiants

DOI: 10.1002/prp2.779 PMID: 34003582 PMC: PMC8130569
pubmed: 34003582
doi: 10.1002/prp2.779
pmc: PMC8130569
doi:

Substances chimiques

ADRB2 protein, human 0
Adrenergic beta-2 Receptor Antagonists 0
Ligands 0
Propanolamines 0
Receptors, Adrenergic, beta-2 0
ICI 118551 46OL1UC10R

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

e00779

Subventions

Organisme : Medical Research Council
ID : MR/N020081/1
Pays : United Kingdom
Organisme : Medical Research Council
ID : MR/N020081/1
Pays : United Kingdom

Informations de copyright

© 2021 The Authors. Pharmacology Research & Perspectives published by John Wiley & Sons Ltd, British Pharmacological Society and American Society for Pharmacology and Experimental Therapeutics.

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Auteurs

Joëlle Goulding (J)

Division of Physiology, Pharmacology and Neuroscience, School of Life Sciences, University of Nottingham, Nottingham, UK.
Centre of Membrane Proteins and Receptors (COMPARE), University of Birmingham and University of Nottingham, Midlands, UK.
ORCID: 0000-0002-6227-4483

Sarah J Mistry (SJ)

Centre of Membrane Proteins and Receptors (COMPARE), University of Birmingham and University of Nottingham, Midlands, UK.
School of Pharmacy, University of Nottingham, Nottingham, UK.
ORCID: 0000-0003-1409-0097

Mark Soave (M)

Division of Physiology, Pharmacology and Neuroscience, School of Life Sciences, University of Nottingham, Nottingham, UK.
Centre of Membrane Proteins and Receptors (COMPARE), University of Birmingham and University of Nottingham, Midlands, UK.
ORCID: 0000-0002-9199-1772

Jeanette Woolard (J)

Division of Physiology, Pharmacology and Neuroscience, School of Life Sciences, University of Nottingham, Nottingham, UK.
Centre of Membrane Proteins and Receptors (COMPARE), University of Birmingham and University of Nottingham, Midlands, UK.
ORCID: 0000-0001-5406-6847

Stephen J Briddon (SJ)

Division of Physiology, Pharmacology and Neuroscience, School of Life Sciences, University of Nottingham, Nottingham, UK.
Centre of Membrane Proteins and Receptors (COMPARE), University of Birmingham and University of Nottingham, Midlands, UK.

Carl W White (CW)

Division of Physiology, Pharmacology and Neuroscience, School of Life Sciences, University of Nottingham, Nottingham, UK.
Centre of Membrane Proteins and Receptors (COMPARE), University of Birmingham and University of Nottingham, Midlands, UK.
Harry Perkins Institute of Medical Research and Centre for Medical Research, University of Western Australia, QEII Medical Centre, Nedlands, Western Australia, Australia.
Australian Research Council Centre for Personalised Therapeutics Technologies, Australia.
ORCID: 0000-0002-4975-6189

Barrie Kellam (B)

Centre of Membrane Proteins and Receptors (COMPARE), University of Birmingham and University of Nottingham, Midlands, UK.
School of Pharmacy, University of Nottingham, Nottingham, UK.
ORCID: 0000-0003-0030-9908

Stephen J Hill (SJ)

Division of Physiology, Pharmacology and Neuroscience, School of Life Sciences, University of Nottingham, Nottingham, UK.
Centre of Membrane Proteins and Receptors (COMPARE), University of Birmingham and University of Nottingham, Midlands, UK.
ORCID: 0000-0002-4424-239X

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Classifications MeSH

questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Effets physiologiques des médicaments › Agents neuromédiateurs › Agents adrénergiques › Antagonistes adrénergiques › Antagonistes bêta-adrénergiques › Antagonistes des récepteurs bêta-2 adrénergiques › Subtype selective fluorescent ligands based on...
questionsmedicales.fr › Phénomènes génétiques › Régulation de l'expression des gènes › Épigenèse génétique › Extinction de l'expression des gènes › Systèmes CRISPR-Cas › Subtype selective fluorescent ligands based on...
questionsmedicales.fr › Phénomènes physiques › Phénomènes optiques › Fluorescence › Subtype selective fluorescent ligands based on...
questionsmedicales.fr › Techniques d'investigation › Techniques génétiques › Génie génétique › Édition de gène › Subtype selective fluorescent ligands based on...
questionsmedicales.fr › Cellules › Cellules épithéliales › Cellules HEK293 › Subtype selective fluorescent ligands based on...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Subtype selective fluorescent ligands based on...
questionsmedicales.fr › Actions chimiques et utilisations › Utilisations spécialisées de produits chimiques › Produits chimiques de laboratoire › Ligands › Subtype selective fluorescent ligands based on...
questionsmedicales.fr › Composés chimiques organiques › Amines › Aminoalcools › Propanolamines › Subtype selective fluorescent ligands based on...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Récepteurs de surface cellulaire › Récepteurs aux neuromédiateurs › Récepteurs catécholaminergiques › Récepteurs adrénergiques › Récepteurs bêta-adrénergiques › Récepteurs bêta-2 adrénergiques › Subtype selective fluorescent ligands based on...