ArticleScientific reports2014
Divergent label-free cell phenotypic pharmacology of ligands at the overexpressed β₂-adrenergic receptors.
Article in Scientific reports, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
What it found
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Who cites it
8 citing papers in PubMed, 20 citations in OpenAlex.
- A Dynamic Mass Redistribution Assay for the Human Sweet Taste Receptor Uncovers G-Protein Dependent Biased Ligands.Frontiers in pharmacology · 2022Article
- Mechanism deconvolution of Qing Fei Pai Du decoction for treatment of Coronavirus Disease 2019 (COVID-19) by label-free integrative pharmacology assays.Journal of ethnopharmacology · 2021Article
- Label-Free Investigations on the G Protein Dependent Signaling Pathways of Histamine Receptors.International journal of molecular sciences · 2021Article
- Label-free high-throughput screening assay for the identification of norepinephrine transporter (NET/SLC6A2) inhibitors.Scientific reports · 2021Article
- Bias analyses of preclinical and clinical D2 dopamine ligands: studies with immediate and complex signaling pathways.The Journal of pharmacology and experimental therapeutics · 2015Article
- New functional activity of aripiprazole revealed: Robust antagonism of D2 dopamine receptor-stimulated Gβγ signaling.Biochemical pharmacology · 2015Article
- Label-free cell phenotypic profiling decodes the composition and signaling of an endogenous ATP-sensitive potassium channel.Scientific reports · 2014Article
- Label-free drug discovery.Frontiers in pharmacology · 2014Review
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
We present subclone sensitive cell phenotypic pharmacology of ligands at the β2-adrenergic receptor (β2-AR) stably expressed in HEK-293 cells. The parental cell line was transfected with green fluorescent protein (GFP)-tagged β2-AR. Four stable subclones were established and used to profile a library of sixty-nine AR ligands. Dynamic mass redistribution (DMR) profiling resulted in a pharmacological activity map suggesting that HEK293 endogenously expresses functional Gi-coupled α2-AR and Gs-coupled β2-AR, and the label-free cell phenotypic activity of AR ligands are subclone dependent. Pathway deconvolution revealed that the DMR of epinephrine is originated mostly from the remodeling of actin microfilaments and adhesion complexes, to less extent from the microtubule networks and receptor trafficking, and certain agonists displayed different efficacy towards the cAMP-Epac pathway. We demonstrate that receptor signaling and ligand pharmacology is sensitive to the receptor expression level, and the organization of the receptor and its signaling circuitry.
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Registered trials
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