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[期刊论文]
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Expression - Level Dependent Activation of Recombinant Human Parathyroid Hormone/Parathyroid Hormone-Related Peptide Receptor: Effect of Human Parathyroid Hormone (1-34), (1-31), and (28-48)
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作 者：
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Oliver Tonn;Sepp Rriegbaum;Andrea Braitmaier;Wolfgang Schäfer;Angelika Esswein;Carola Dony;Klaus Kaluza;Konrad Honold;
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出版年：2000
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页 码：133 - 151
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出版社：Taylor And Francis
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摘 要：
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A stable recombinant Chinese hamster ovary (CHO) cell model system expressing the human type-1 receptor for parathyroid hormone and parathyroid hormone-related peptide (hPTH-R) was established for the analysis of human PTH (hPTH) variants. The cell lines showed receptor expression in the range from 105 to 1.9xl06 receptors per cell. The affinity of the receptors for hPTH-(l-34) was independent of the receptor number per cell (K2xl05 receptors per cell and Ca++ signals were maximal in cell lines expressing >1.4xl06 receptors per cell. Second messenger specific inhibitors demonstrated that PTH-induced increases in intracellular cAMP and Ca++ are independent and Ca++ ions are derived from intracellular stores. The cAMP-specific receptor activator hPTH-(l-31) showed also an increase in intracellular Ca++. Even in cell lines expressing more than 10 receptors per cell the Ca++/PKC specific activator hPTH-(28-48) did not activate hPTH-Rs. Based on these results, synthesis of further derivatives of PTH is required to identify pathway-specific ligands for the type-1 hPTH-R.
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所属期刊
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ISSN: 1079-9893
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来自：Taylor And Francis
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