Receptor-Drug  Interaction: Europium Employment for Studying the Biochemical Pathway of  G-Protein-Coupled Receptor Activation

Antonio, Colabufo Nicola; Grazia, Perrone Maria; Marialessandra, Contino; Francesco, Berardi; Roberto, Perrone

doi:https://doi.org/10.1155/2007/12635

Metal-Based Drugs

On this page

Abstract References Copyright Related Articles

Review Article | Open Access

Volume 2007 | Article ID 012635 | https://doi.org/10.1155/2007/12635

Receptor-Drug Interaction: Europium Employment for Studying the Biochemical Pathway of G-Protein-Coupled Receptor Activation

Colabufo Nicola Antonio,¹Perrone Maria Grazia,¹Contino Marialessandra,¹Berardi Francesco,¹and Perrone Roberto¹

Academic Editor: Irena Kostova

Received26 Oct 2007

Accepted11 Dec 2007

Published25 Feb 2008

Abstract

In medicinal chemistry field, the biochemical pathways, involved in 7-transmembrane domains G-protein coupled receptors (GPCRs) activation, are commonly studied to establish the activity of ligands towards GPCRs. The most studied steps are the measurement of activated GTP-α subunit and stimulated intracellular cAMP. At the present, many researchers defined agonist or antagonist activity of potential GPCRs drugs employing [35S]GTPγS or [3H]cAMP as probes. Recently, the corresponding lanthanide labels Eu-GTP and Eu-cAMP as alternative to radiochemicals have been developed because they are highly sensitive, easy to automate, easily synthesized, they display a much longer shelf-life and they can be used in multilabel experiments. In the present review, the receptor-drug interaction by europium employment for studying the biochemical pathway of GPCR activation has been focused. Moreover, comparative studies between lanthanide label probes and the corresponding radiolabeled compounds have been carried out.

References

S. V. Beltyukova, E. I. Tselik, and A. V. Egorova, “Use of sensitized luminescence of lanthanides in analysis of drugs,” Journal of Pharmaceutical and Biomedical Analysis, vol. 18, no. 1-2, pp. 263–266, 1998.
View at: Publisher Site | Google Scholar
I. Hemmilä and V. Laitala, “Progress in lanthanides as luminescent probes,” Journal of Fluorescence, vol. 15, no. 4, pp. 529–542, 2005.
View at: Publisher Site | Google Scholar
H. L. Handl and R. J. Gillies, “Lanthanide-based luminescent assays for ligand-receptor interactions,” Life Sciences, vol. 77, no. 4, pp. 361–371, 2005.
View at: Publisher Site | Google Scholar
A. Scorilas and E. P. Diamandis, “Polyvinylamine-streptavidin complexes labeled with a europium chelator: a universal detection reagent for solid-phase time resolved fluorometric applications,” Clinical Biochemistry, vol. 33, no. 5, pp. 345–350, 2000.
View at: Publisher Site | Google Scholar
E. F. Gudgin Dickson, A. Pollak, and E. P. Diamandis, “Ultrasensitive bioanalytical assays using time-resolved fluorescence detection,” Pharmacology & Therapeutics, vol. 66, no. 2, pp. 207–235, 1995.
View at: Publisher Site | Google Scholar
E. F. Gudgin Dickson, A. Pollak, and E. P. Diamandis, “Time-resolved detection of lanthanide luminescence for ultrasensitive bioanalytical assays,” Journal of Photochemistry and Photobiology B, vol. 27, no. 1, pp. 3–19, 1995.
View at: Publisher Site | Google Scholar
E. F. Gudgin Dickson, “Enzyme-amplified lanthanide luminescence for detection of enzyme labels in ultrasensitive bioanalytical assays,” Journal of Photochemistry and Photobiology B, vol. 17, no. 3, pp. 293–294, 1993.
View at: Publisher Site | Google Scholar
M. Xiao and P. R. Selvin, “Quantum yields of luminescent lanthanide chelates and far-red dyes measured by resonance energy transfer,” Journal of the American Chemical Society, vol. 123, no. 29, pp. 7067–7073, 2001.
View at: Publisher Site | Google Scholar
R. T. Lee and Y. C. Lee, “A derivative of diethylenetriaminepentaacetic acid for europium labeling of proteins,” Bioconjugate Chemistry, vol. 12, no. 6, pp. 845–849, 2001.
View at: Publisher Site | Google Scholar
A. Lobnik, N. Majcen, K. Niederreiter, and G. Uray, “Optical pH sensor based on the absorption of antenna generated europium luminescence by bromothymolblue in a sol-gel membrane,” Sensors and Actuators B, vol. 74, no. 1–3, pp. 200–206, 2001.
View at: Publisher Site | Google Scholar
G. E. Khalil, K. Lau, and G. D. Phelan et al., “Europium $β$ -diketonate temperature sensors: effects of ligands, matrix, and concentration,” Review of Scientific Instruments, vol. 75, no. 1, pp. 192–206, 2004.
View at: Publisher Site | Google Scholar
S.-H. Li, W.-T. Yuan, C.-Q. Zhu, and J.-G. Xu, “Species-differentiable sensing of phosphate-containing anions in neutral aqueous solution based on coordinatively unsaturated lanthanide complex probes,” Analytical Biochemistry, vol. 331, no. 2, pp. 235–242, 2004.
View at: Publisher Site | Google Scholar
M. Schäferling, M. Wu, and O. S. Wolfbeis, “Time-resolved fluorescent imaging of glucose,” Journal of Fluorescence, vol. 14, no. 5, pp. 561–568, 2004.
View at: Publisher Site | Google Scholar
M. Wu, Z. Lin, and O. S. Wolfbeis, “Determination of the activity of catalase using a europium(III)-tetracycline-derived fluorescent substrate,” Analytical Biochemistry, vol. 320, no. 1, pp. 129–135, 2003.
View at: Publisher Site | Google Scholar
J. C. DiCesare, J. Parker, S. N. Horne, J. Kita, R. Earni, and C. Peeples, “Progress in developing nerve agent sensors using combinatorial techniques,” in Materials Research Society Symposium Proceedings, vol. 787, pp. 17–22, Boston, Mass, USA, December 2003.
View at: Google Scholar
A. M. Casas-Hernández, M. P. Aguilar-Caballos, and A. Gómez-Hens, “Application of time-resolved luminescence methodology to the determination of phthalate esters,” Analytical Letters, vol. 36, no. 5, pp. 1017–1027, 2003.
View at: Publisher Site | Google Scholar
H. Frang, V.-M. Mukkala, and R. Syystö et al., “Nonradioactive GTP binding assay to monitor activation of G-protein-coupled receptors,” Assay and Drug Development Technologies, vol. 1, no. 2, pp. 275–280, 2003.
View at: Publisher Site | Google Scholar
M. Engström, A. Närvänen, J.-M. Savola, and S. Wurster, “Assessing activation of the human neuropeptide FF2 receptor with a non-radioactive GTP binding assay,” Peptides, vol. 25, no. 12, pp. 2099–2104, 2004.
View at: Publisher Site | Google Scholar
M. Leopoldo, E. Lacivita, N. A. Colabufo, M. Contino, F. Berardi, and R. Perrone, “First structure-activity relationship study on dopamine $D_{3}$ receptor agents with $N$ -[4-(4-arylpiperazin-1-yl)butyl]-arylcarboxamide structure,” Journal of Medicinal Chemistry, vol. 48, no. 25, pp. 7919–7922, 2005.
View at: Publisher Site | Google Scholar
M. C. Coldwell, I. Boyfield, A. M. Brown, G. Stemp, and D. N. Middlemiss, “Pharmacological characterization of extracellular acidification rate responses in human $D_{2 (long)}$ , $D_{3}$ and $D_{4 \cdot 4}$ receptors expressed in Chinese hamster ovary cells,” British Journal of Pharmacology, vol. 127, no. 5, pp. 1135–1144, 1999.
View at: Publisher Site | Google Scholar
C. Stratowa, A. Himmler, and A. P. Czernilofsky, “Use of a luciferase reporter system for characterizing G-protein-linked receptors,” Current Opinion in Biotechnology, vol. 6, no. 5, pp. 574–581, 1995.
View at: Publisher Site | Google Scholar
C. M. Suto and D. M. Ignar, “Selection of an optimal reporter gene for cell-based high throughput screening assays,” Journal of Biomolecular Screening, vol. 2, no. 1, pp. 7–9, 1997.
View at: Publisher Site | Google Scholar
A. S. Goetz, J. L. Andrews, T. R. Littleton, and D. M. Ignar, “Development of a facile method for high throughput screening with reporter gene assays,” Journal of Biomolecular Screening, vol. 5, no. 5, pp. 377–384, 2000.
View at: Publisher Site | Google Scholar
I. Kariv, M. E. Stevens, D. L. Behrens, and K. R. Oldenburg, “High throughput quantitation of cAMP production mediated by activation of seven transmembrane domain receptors,” Journal of Biomolecular Screening, vol. 4, no. 1, pp. 27–32, 1999.
View at: Publisher Site | Google Scholar
L. J. Emorine, S. Marullo, and M.-M. Briend-Sutren et al., “Molecular characterization of the human $β_{3}$ -adrenergic receptor,” Science, vol. 245, no. 4922, pp. 1118–1121, 1989.
View at: Publisher Site | Google Scholar
M. G. Perrone, E. Santandrea, and L. Bleve et al., “Stereospecific synthesis and bio-activity of novel $β_{3}$ -adrenoceptor agonists and inverse agonists,” to appear in Bioorganic & Medicinal Chemistry.
View at: Publisher Site | Google Scholar
G. Jin, A. Aulabaugh, J. Pocas, H. Liu, R. Kriz, and D. Sampath, “Development and comparison of nonradioactive in vitro kinase assays for NIMA-related kinase 2,” Analytical Biochemistry, vol. 358, no. 1, pp. 59–69, 2006.
View at: Publisher Site | Google Scholar
D. Waddleton, C. Ramachandran, and Q. Wang, “Development of a time-resolved fluorescent assay for measuring tyrosine-phosphorylated proteins in cells,” Analytical Biochemistry, vol. 309, no. 1, pp. 150–157, 2002.
View at: Publisher Site | Google Scholar
M. S. Hayden and S. Ghosh, “Signaling to NF- $κ$ B,” Genes & Development, vol. 18, no. 18, pp. 2195–2224, 2004.
View at: Publisher Site | Google Scholar
M. Karin and F. R. Greten, “NF- $κ$ B: linking inflammation and immunity to cancer development and progression,” Nature Reviews Immunology, vol. 5, no. 10, pp. 749–759, 2005.
View at: Publisher Site | Google Scholar
D. S. Bassères and A. S. Baldwin, “Nuclear factor- $κ$ B and inhibitor of $κ$ B kinase pathways in oncogenic initiation and progression,” Oncogene, vol. 25, no. 51, pp. 6817–6830, 2006.
View at: Google Scholar
G. Bonizzi and M. Karin, “The two NF- $κ$ B activation pathways and their role in innate and adaptive immunity,” Trends in Immunology, vol. 25, no. 6, pp. 280–288, 2004.
View at: Publisher Site | Google Scholar
S. Janssens and J. Tschopp, “Signals from within: the DNA-damage-induced NF- $κ$ B response,” Cell Death & Differentiation, vol. 13, no. 5, pp. 773–784, 2006.
View at: Publisher Site | Google Scholar
T. M. Sadler, M. Achilleos, and S. Ragunathan et al., “Development and comparison of two nonradioactive kinase assays for I $κ$ B kinase,” Analytical Biochemistry, vol. 326, no. 1, pp. 106–113, 2004.
View at: Publisher Site | Google Scholar

Copyright

Copyright © 2007 Colabufo Nicola Antonio et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

PDF Download Citation Order printed copies

Views

295

Downloads

95

Citations