Detection of receptor ligands by monitoring selective stabilization of a Renilla luciferase-tagged, constitutively active mutant, G-protein-coupled receptor

British Journal of Pharmacology

Volumn 133, Issue 2, 2001, Pages 315-323

  Ramsay, Douglas ^a   Bevan, Nicola ^b   Rees, Stephen ^b   Milligan, Graeme ^a  

^a UNIVERSITY OF GLASGOW   (United Kingdom)

^b GLAXOSMITHKLINE   (United Kingdom)

Author keywords

Adrenoceptor; Constitutive activity; G protein coupled receptor; Ligand screening; Luciferase

Indexed keywords

ADENYLATE CYCLASE; BETA 2 ADRENERGIC RECEPTOR; G PROTEIN COUPLED RECEPTOR; GREEN FLUORESCENT PROTEIN; ISOPRENALINE; LIGAND; LUCIFERASE;

ARTICLE; CARBOXY TERMINAL SEQUENCE; CONFORMATIONAL TRANSITION; ENZYME ACTIVITY; HUMAN; HUMAN CELL; INTERNALIZATION; LIGAND BINDING; PRIORITY JOURNAL; PROTEIN ANALYSIS; PROTEIN EXPRESSION; RENILLA RENIFORMIS;

EID: 0034986205     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0704077     Document Type: Article

References (29)

1. 2 receptor
2. Internal trafficking and surface mobility of a functionally intact beta2-adrenergic receptor-green fluorescent protein conjugate
3. Use of constitutive G protein-coupled receptor activity for drug discovery
4. Structural instability of a constitutively active G protein-coupled receptor. Agonist-independent activation due to conformational flexibility
5. Agonists induce conformational changes in transmembrane domains III and VI of the beta2 adrenoceptor
6. Synergism of constitutive activity in alpha 1-adrenergic receptor activation
7. Constitutive activation of the beta2 adrenergic receptor alters the orientation of its sixth membrane-spanning segment
8. Using green fluorescent proteins to study G-protein-coupled receptor localization and trafficking
9. Visualization of agonist-induced sequestration and down-regulation of a green fluorescent protein-tagged β2-adrenergic receptor
10. Up-regulation of the levels of expression and function of a constitutively active mutant of the hamster alphal B-adrenoceptor by ligands that act as inverse agonists
11. Constitutive activity of receptors coupled to guanine-nucleotide regulatory proteins
12. Agonist-independent regulation of constitutively active G- protein-coupled receptors
13. 2-adrenoceptor in transfected neuroblastoma x glioma hybrid cells
14. 2-adrenoceptor-green fluorescent protein fusion proteins
15. 2-adrenoceptors; comparisons with the unmodified receptors
16. Regulation of spontaneous activity of the δ-opioid receptor: Studies of inverse agonism in intact cells
17. Exploring the dynamics of regulation of G protein-coupled receptors using green fluorescent protein
18. Inverse agonism and the regulation of receptor number
19. Inverse agonism: Pharmacological curiosity or potential therapeutic strategy?
20. Review: Amino acid domains involved in constitutive activation of G-protein-coupled receptors
21. A constitutively active mutant beta 2-adrenergic receptor is constitutively desensitized and phosphorylated
22. Reporter gene systems for the study of G protein-coupled receptor signal transduction in mammalian cells
23. 2-adrenergic receptor-extending the ternary complex model
24. Negative antagonists promote an inactive conformation of the beta 2-adrenergic receptor
25. Constitutively active G protein-coupled receptors: Potential mechanisms of receptor activation
26. 1b-adrenoceptor
27. i assays in transfected cells
28. Following cell fate in the living mouse embryo
29. Inverse agonism and neutral antagonism at a constitutively active alpha-la adrenoceptor