Fluorescence Correlation Spectroscopy in Drug Discovery : Study of Alexa532-Endothelin 1 Binding to the Endothelin ETA Receptor to Describe the Pharmacological Profile of Natural Products
Joint Authors
Häberlein, Hanns
Bolaños, Jessica
Raja, Huzefa
Caballero-George, Catherina
Jakobs, Daniel
Shearer, Carol
Bermingham, Eldredge
Sorkalla, Thomas
Source
Issue
Vol. 2012, Issue 2012 (31 Dec. 2012), pp.1-7, 7 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2012-05-01
Country of Publication
Egypt
No. of Pages
7
Main Subjects
Natural & Life Sciences (Multidisciplinary)
Medicine
Information Technology and Computer Science
Abstract EN
Fluorescence correlation spectroscopy and the newly synthesized Alexa532-ET1 were used to study the dynamics of the endothelin ETA receptor-ligand complex alone and under the influence of a semisynthetic selective antagonist and a fungal extract on living A10 cells.
Dose-dependent increase of inositol phosphate production was seen for Alexa532-ET1, and its binding was reduced to 8% by the selective endothelin ETA antagonist BQ-123, confirming the specific binding of Alexa532-ET1 to the endothelin ETA receptor.
Two different lateral mobilities of the receptor-ligand complexes within the cell membrane were found allowing the discrimination of different states for this complex.
BQ-123 showed a strong binding affinity to the “inactive” receptor state characterized by the slow diffusion time constant.
A similar effect was observed for the fungal extract, which completely displaced Alexa532-ET1 from its binding to the “inactive” receptor state.
These findings suggest that both BQ-123 and the fungal extract act as inverse agonists.
American Psychological Association (APA)
Caballero-George, Catherina& Sorkalla, Thomas& Jakobs, Daniel& Bolaños, Jessica& Raja, Huzefa& Shearer, Carol…[et al.]. 2012. Fluorescence Correlation Spectroscopy in Drug Discovery : Study of Alexa532-Endothelin 1 Binding to the Endothelin ETA Receptor to Describe the Pharmacological Profile of Natural Products. The Scientific World Journal،Vol. 2012, no. 2012, pp.1-7.
https://search.emarefa.net/detail/BIM-478503
Modern Language Association (MLA)
Caballero-George, Catherina…[et al.]. Fluorescence Correlation Spectroscopy in Drug Discovery : Study of Alexa532-Endothelin 1 Binding to the Endothelin ETA Receptor to Describe the Pharmacological Profile of Natural Products. The Scientific World Journal No. 2012 (2012), pp.1-7.
https://search.emarefa.net/detail/BIM-478503
American Medical Association (AMA)
Caballero-George, Catherina& Sorkalla, Thomas& Jakobs, Daniel& Bolaños, Jessica& Raja, Huzefa& Shearer, Carol…[et al.]. Fluorescence Correlation Spectroscopy in Drug Discovery : Study of Alexa532-Endothelin 1 Binding to the Endothelin ETA Receptor to Describe the Pharmacological Profile of Natural Products. The Scientific World Journal. 2012. Vol. 2012, no. 2012, pp.1-7.
https://search.emarefa.net/detail/BIM-478503
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-478503