期刊
SCIENTIFIC WORLD JOURNAL
卷 -, 期 -, 页码 -出版社
HINDAWI LTD
DOI: 10.1100/2012/524169
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资金
- National Secretariat of Science, Technology and Innovation (SENACYT) from the Panamanian government [COL06-006, COL08-014]
- International Foundation for Science (Stockholm, Sweden)
- Organization for the Prohibition of Chemical Weapons (The Hague, The Netherlands) [F/4907-1]
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.
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