ReferenceID 5096
A novel β2-AR agonist, Higenamine, induces β-arrestin-biased signaling
Sci China Life Sci
The biased ligands in G protein-coupled receptors (GPCRs) have opened new avenues for developing safer and more effective drugs. However, the identification of such biased ligands as drug candidates is highly desirable.
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Record Fields
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- Reference Id
- 5096
- Evidence Id
- 21686
- Core Evidence Id
- 21686
- Source Reference Id
- 3481
- Herb2 Reference Id
- HBREF004278
- Subject Paper Key
- HBIN023239_34783996
- Pubmed Id
- 34783996
- Doi
- 10.1007/s11427-021-2008-1
- Paper Title
- A novel β2-AR agonist, Higenamine, induces β-arrestin-biased signaling
- Paper Abstract
- The biased ligands in G protein-coupled receptors (GPCRs) have opened new avenues for developing safer and more effective drugs. However, the identification of such biased ligands as drug candidates is highly desirable. Here, we report that Higenamine, a compound isolated from a Chinese herb, functions as a novel beta-arrestin-biased ligand of the beta2-adrenergic receptor (beta2-AR). The radioligand binding assays demonstrated that Higenamine was the ligand of beta2-AR. Higenamine induced phosphorylation of extracellular signal-regulated kinase 1/2 (ERK1/2), which can be blocked by propranolol, an inhibitor of beta2-AR. The Gi protein inhibitor, pertussis toxin, had no effect on the phosphorylation of ERK1/2 induced by Higenamine. Furthermore, Higenamine induced ERK1/2 phosphorylation through transactivation of Epithelial growth factor receptor (EGFR). We also found that Higenamine-induced-ERK1/2 phosphorylation is dependent on beta-arrestin1/2, and HG inhibits Doxorubicin-induced cardiomyocyte apoptosis. Our results identify Higenamine as a novel biased ligand via the beta-arrestin-dependent pathway. These findings give us a better understanding of Higenamine's potential role in designing diagnostic and therapeutic strategies.
- Journal
- Sci China Life Sci
- Publish Year
- 2021
- Experiment Subject
- Experiment Type
- Cell Experiment
- Phenotype Related
- Paper Title Cn
- Paper Title En
- A novel β2-AR agonist, Higenamine, induces β-arrestin-biased signaling
- Bilingual Status
- semi_complete