Discovery and characterization of [H]8-OH-DPAT binding to HeLaS3 cells |
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Authors: | Jin-Jye Feng Fong-Chi Cheng Jiann-Wu Wei |
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Institution: | a Institute of Molecular and Cellular Biology, National Tsing Hua University, 101, Section 2, Kuang-Fu Road, Hsinchu 30013, Taiwan, ROC b Biochemical Pharmacology Lab, MDS Pharma Services Taiwan, Ltd., 158 Li-Teh Road, Peitou, Taipei 112, Taiwan, ROC |
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Abstract: | 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. |
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Keywords: | [3H]8-OH-DPAT 5-HT1A receptor GPCRs HeLaS3 Radioligand binding assay |
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