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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Heitman, L. H. Nederpelt, I. IJzerman, A. P. Vergroesen, R. D. |
| Description | Country affiliation: Netherlands Author Affiliation: Nederpelt I ( Division of Medicinal Chemistry, Leiden Academic Centre for Drug Research (LACDR), Leiden University, P.O. Box 9502, 2300 RA Leiden, The Netherlands.); Vergroesen RD ( Division of Medicinal Chemistry, Leiden Academic Centre for Drug Research (LACDR), Leiden University, P.O. Box 9502, 2300 RA Leiden, The Netherlands.); IJzerman AP ( Division of Medicinal Chemistry, Leiden Academic Centre for Drug Research (LACDR), Leiden University, P.O. Box 9502, 2300 RA Leiden, The Netherlands. Electronic address: ijzerman@lacdr.leidenuniv.nl.); Heitman LH ( Division of Medicinal Chemistry, Leiden Academic Centre for Drug Research (LACDR), Leiden University, P.O. Box 9502, 2300 RA Leiden, The Netherlands.) |
| Abstract | The gonadotropin-releasing hormone (GnRH) receptor is a drug target for certain hormone-dependent diseases such as prostate cancer. In this study, we examined the activation profiles of the endogenous ligand, GnRH and a well-known marketed analog, buserelin using a label-free assay in pituitary T3-1 cells with endogenous GnRH receptor expression. This whole cell impedance-based technology allows for the real-time measurement of morphological cellular changes. Both agonists dose-dependently decreased the impedance as a result of GnRH receptor activation with potencies of 9.3 ± 0.1 (pEC50 value, buserelin) and 7.8 ± 0.06 (pEC50 value, GnRH). Subsequently, GnRH receptor activation was completely abolished with a selective G q inhibitor, thereby confirming the G q-coupling of the GnRH receptor in pituitary T3-1 cells. Additionally, we observed continued responses after agonist stimulation of T3-1 cells indicating long-lasting cellular effects. Wash-out experiments demonstrated that the long-lasting effects induced by GnRH were most likely caused by rebinding since over 70% of the original response was abolished after wash-out. In contrast, a long receptor residence time was responsible for the prolonged effects caused by buserelin, with over 70% of the original response remaining after wash-out. In summary, we validated that impedance-based label-free technology is suited for studying receptor-mediated activation in cell lines endogenously expressing the target of interest. Moreover, this real-time monitoring allows the examination of binding kinetics and its influence on receptor activation at a cellular level. |
| ISSN | 09565663 |
| Volume Number | 79 |
| e-ISSN | 18734235 |
| Journal | Biosensors and Bioelectronics |
| Language | English |
| Publisher | Elsevier |
| Publisher Date | 2016-05-15 |
| Publisher Place | Great Britain (UK) |
| Access Restriction | One Nation One Subscription (ONOS) |
| Subject Keyword | Pituitary Gland Metabolism Receptors, Lhrh Biosensing Techniques Buserelin Pharmacology Cell Line Electric Impedance Humans Inositol Phosphates Cytology Drug Effects Agonists Journal Article Research Support, Non-u.s. Gov't Discipline Biotechnology |
| Content Type | Text |
| Resource Type | Article |
| Subject | Nanoscience and Nanotechnology Medicine Biophysics Biomedical Engineering Biotechnology Electrochemistry |
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