Miniatura

Fitxers

573505.pdf (518.28 KB)

Tipus de document

Article

Versió

Versió acceptada

Data de publicació

2009-12-15

Tots els drets reservats

Si us plau utilitzeu sempre aquest identificador per citar o enllaçar aquest document: https://hdl.handle.net/2445/127978

Useful pharmacological parameters for G-protein-coupled receptor homodimers obtained from competition experiments. Agonist-antagonist binding modulation

Títol de la revista

Autors

Director/Tutor

ISSN de la revista

Títol del volum

Recurs relacionat

https://doi.org/10.1016/j.bcp.2009.07.012

Resum

Many G-protein-coupled receptors (GPCRs) are expressed on the plasma membrane as dimers. Since drug binding data are currently fitted using equations developed for monomeric receptors, the interpretation of the pharmacological data are equivocal in many cases. As reported here, GPCR dimer models account for changes in competition curve shape as a function of the radioligand concentration used, something that cannot be explained by monomeric receptor models. Macroscopic equilibrium dissociation constants for the agonist and homotropic cooperativity index reflecting the intramolecular communication within the dopamine D1 or adenosine A2A receptor homodimer as well as hybrid equilibrium dissociation constant, which reflects the antagonist/agonist modulation may be calculated by fitting binding data from antagonist/agonist competition experiments to equations developed from dimer receptor models. Comparing fitting the data by assuming a classical monomeric receptor model or a dimer model, it is shown that dimer receptor models provide more clues useful in drug discovery than monomer-based models.

Matèries

Bioquímica, Biologia molecular, Interacció cel·lular

Matèries (anglès)

Biochemistry, Molecular biology, Cell interaction

Citació

Col·leccions

Articles publicats en revistes (Bioquímica i Biomedicina Molecular)

Citació

CASADÓ, Vicent, FERRADA, Carla, BONAVENTURA, Jordi, GRACIA, Eduard, MALLOL MONTERO, Josefa, CANELA CAMPOS, Enric i. (enric isidre), LLUÍS I BISET, Carme, CORTÉS TEJEDOR, Antonio, FRANCO FERNÁNDEZ, Rafael. Useful pharmacological parameters for G-protein-coupled receptor homodimers obtained from competition experiments. Agonist-antagonist binding modulation. _Biochemical Pharmacology_. 2009. Vol. 78, núm. 12, pàgs. 1456-1463. [consulta: 23 de gener de 2026]. ISSN: 0006-2952. [Disponible a: https://hdl.handle.net/2445/127978]

Exportar metadades

JSON - METS

Compartir registre