dc.contributor.author | Caballero-George, Catherina | en |
dc.contributor.author | Sorkalla, Thomas | en |
dc.contributor.author | Jakobs, Daniel | en |
dc.contributor.author | Bolanos, Jessica | en |
dc.contributor.author | Raja, Huzefa | en |
dc.contributor.author | Shearer, Carol | en |
dc.contributor.author | Bermingham, Eldredge | en |
dc.contributor.author | Haeberlein, Hanns | en |
dc.date.accessioned | 2013-09-06T19:17:38Z | |
dc.date.available | 2013-09-06T19:17:38Z | |
dc.date.issued | 2012 | |
dc.identifier.citation | Caballero-George, Catherina, Sorkalla, Thomas, Jakobs, Daniel, Bolanos, Jessica, Raja, Huzefa, Shearer, Carol, Bermingham, Eldredge, and Haeberlein, Hanns. 2012. "<a href="https%3A%2F%2Frepository.si.edu%2Fhandle%2F10088%2F21220">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</a>." <em>Scientific World Journal</em>. 524169–524169. <a href="https://doi.org/10.1100/2012/524169">https://doi.org/10.1100/2012/524169</a> | en |
dc.identifier.issn | 1537-744X | |
dc.identifier.uri | http://hdl.handle.net/10088/21220 | |
dc.description.abstract | 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. | en |
dc.relation.ispartof | Scientific World Journal | en |
dc.title | Fluorescence Correlation Spectroscopy in Drug Discovery: Study of Alexa532-Endothelin 1 Binding to the Endothelin ET<SUB>A</SUB> Receptor to Describe the Pharmacological Profile of Natural Products | en |
dc.type | Journal Article | en |
dc.identifier.srbnumber | 112001 | |
dc.identifier.doi | 10.1100/2012/524169 | |
rft.jtitle | Scientific World Journal | |
rft.spage | 524169 | |
rft.epage | 524169 | |
dc.description.SIUnit | Peer-Reviewed | en |
dc.description.SIUnit | STRI | en |
dc.citation.spage | 524169 | |
dc.citation.epage | 524169 |