Discovery and characterization of [3H]8-OH-DPAT binding to HeLaS3 cells
Autor: | Chun-Hsiung Lin, Jiann-Wu Wei, Shiaw-Der Yang, Fong-Chi Cheng, Jin-Jye Feng |
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Rok vydání: | 2009 |
Předmět: |
Agonist
8-Hydroxy-2-(di-n-propylamino)tetralin medicine.drug_class Biophysics Biology Serotonergic Biochemistry Binding Competitive Rhodopsin-like receptors Receptors G-Protein-Coupled Serotonin Receptor Agonists Radioligand Assay Receptor Serotonin 5-HT1A medicine Humans Dimethyl Sulfoxide Serotonin Binding site Receptor Molecular Biology 5-HT receptor G protein-coupled receptor HeLa Cells |
Zdroj: | Archives of biochemistry and biophysics. 495(1) |
ISSN: | 1096-0384 |
Popis: | Some G protein-coupled receptors (GPCRs) have functional links to cancer biology, yet the manifestation of GPCRs in tumor types is little studied to date. Using a battery of radioligand binding assays, we sought to characterize GPCR recognition binding sites on HeLaS3 tumor cells. High levels of binding of the selective serotonin 5-HT1A receptor agonist [3H]8-OH-DPAT were observed in these cells. Saturation and homologous competition experiments indicated that [3H]8-OH-DPAT bound different populations of high- and low-affinity sites. In competition experiments, several serotonergic compounds displaced [3H]8-OH-DPAT binding with low potency from its high-affinity binding sites, suggesting that low-affinity binding is the predominant mode of binding. A variety of drugs targeting different classes of receptors did not affect [3H]8-OH-DPAT binding. These observations may help elucidate the pathophysiological and functional relevance of 5-HT receptors in tumor cells and link GPCRs and tumorigenic mechanisms to pharmacological and chemotherapeutic paradigms. |
Databáze: | OpenAIRE |
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