ArticleScientific reports2015
Luciferase reporter gene assay on human 5-HT receptor: which response element should be chosen?
Article in Scientific reports, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 21 citations in OpenAlex.
- Enhancement of a nuclear factor of activated T cells (NFAT) reporter for the study of G protein-coupled receptors.Communications biology · 2026Article
- Re-evaluating Gα protein-response element specificity in GPCR signaling.Communications biology · 2026Article
- Biased signalingActa pharmaceutica Sinica. B · 2025Review
- The cell adhesion molecule CD44 acts as a modulator of 5-HT7 receptor functions.Cell communication and signaling : CCS · 2024Article
- ACBD3 modulates KDEL receptor interaction with PKA for its trafficking via tubulovesicular carrier.BMC biology · 2021Article
- Ferulic acid alleviates abnormal behaviors in isolation-reared mice via 5-HTPsychopharmacology · 2021Article
- Complementary roles of murine NaScientific reports · 2020Article
- Potency, efficacy, and selectivity of GR64349 at human recombinant neurokinin NK2 and NK1 receptors.Neuroscience letters · 2019Article
- Ligand-induced activation of ERK1/2 signaling by constitutively active GActa pharmacologica Sinica · 2019Article
- Melatonin receptor agonistExperimental and therapeutic medicine · 2019Article
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Serotonin (5-HT) receptors are valuable molecular targets for antipsychotic drug discovery. Current reported methods for detecting 5-HT receptors, such as cAMP accumulation and calcium influx assay, are often demanding specialized instruments and inconvenient. The luciferase reporter gene assay, based on the responsible-element-regulated expression of luciferase, has been widely applied in the high-throughput functional assay for many targets because of its high sensitivity and reliability. However, 5-HT receptors couple to multiple G-proteins regulate respective downstream signalling pathways and are usually detected using different response elements. Hence, finding a suitable response element to fulfil the detection of different 5-HT receptors and make the results of luciferase reporter gene assays generalizable is very useful for active compounds screening. Here, we conducted three luciferase reporter assays using CRE, NFAT, and SRE response elements attached to 5-HT to detect the activation of different 5-HT receptors in CHO-K1 cells. The potencies and efficacies of the reported ligands (agonists and antagonists) were determined and compared. Our results indicate that CRE-luciferase reporter gene is sensitive and reliable to detect the activities of G protein-coupled 5-HT receptors.
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