| 20018167 |
Feng JJ, Cheng FC, Lin CH, Wei JW, Yang SD: Discovery and characterization of [3H] 8-OH-DPAT binding to HeLaS3 cells. Arch Biochem Biophys. 2010 Mar 1;495(1):14-20. Epub 2009 Dec 16.
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-HT (1A) 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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