Expression of EGFP-amino-tagged human mu opioid receptor in Drosophila Schneider 2 cells: a potential expression system for large-scale production of G-protein coupled receptors

2003 ◽  
Vol 31 (1) ◽  
pp. 123-132 ◽  
Author(s):  
Bénédicte G Perret ◽  
Renaud Wagner ◽  
Sandra Lecat ◽  
Karl Brillet ◽  
Gwénaël Rabut ◽  
...  
Keyword(s):  
G Protein ◽  
Opioid Receptor ◽  
Large Scale ◽  
Expression System ◽  
Mu Opioid Receptor ◽  
G Protein Coupled Receptors ◽  
Scale Production ◽  
Mu Opioid ◽  
Large Scale Production ◽  
G Protein Coupled

scholarly journals Measuring ligand efficacy at the mu-opioid receptor using a conformational biosensor

eLife ◽  
2018 ◽  
Vol 7 ◽  
Author(s):  
Kathryn E Livingston ◽  
Jacob P Mahoney ◽  
Aashish Manglik ◽  
Roger K Sunahara ◽  
John R Traynor
Keyword(s):  
G Protein ◽  
Opioid Receptor ◽  
Mu Opioid Receptor ◽  
G Protein Coupled Receptors ◽  
Physiological Effects ◽  
Allosteric Modulators ◽  
Mu Opioid ◽  
Class A ◽  
Orthosteric Ligands ◽  
G Protein Coupled

The intrinsic efficacy of orthosteric ligands acting at G-protein-coupled receptors (GPCRs) reflects their ability to stabilize active receptor states (R*) and is a major determinant of their physiological effects. Here, we present a direct way to quantify the efficacy of ligands by measuring the binding of a R*-specific biosensor to purified receptor employing interferometry. As an example, we use the mu-opioid receptor (µ-OR), a prototypic class A GPCR, and its active state sensor, nanobody-39 (Nb39). We demonstrate that ligands vary in their ability to recruit Nb39 to µ-OR and describe methadone, loperamide, and PZM21 as ligands that support unique R* conformation(s) of µ-OR. We further show that positive allosteric modulators of µ-OR promote formation of R* in addition to enhancing promotion by orthosteric agonists. Finally, we demonstrate that the technique can be utilized with heterotrimeric G protein. The method is cell-free, signal transduction-independent and is generally applicable to GPCRs.

scholarly journals A Computationally Designed Water-Soluble Variant of a G-Protein-Coupled Receptor: The Human Mu Opioid Receptor

PLoS ONE ◽  
2013 ◽  
Vol 8 (6) ◽  
pp. e66009 ◽  
Author(s):  
Jose Manuel Perez-Aguilar ◽  
Jin Xi ◽  
Felipe Matsunaga ◽  
Xu Cui ◽  
Bernard Selling ◽  
...  
Keyword(s):  
G Protein ◽  
Opioid Receptor ◽  
Mu Opioid Receptor ◽  
Water Soluble ◽  
G Protein Coupled Receptor ◽  
Mu Opioid ◽  
G Protein Coupled

scholarly journals Large-scale production and study of a synthetic G protein-coupled receptor: Human olfactory receptor 17-4

2009 ◽  
Vol 106 (29) ◽  
pp. 11925-11930 ◽  
Author(s):  
B. L. Cook ◽  
D. Steuerwald ◽  
L. Kaiser ◽  
J. Graveland-Bikker ◽  
M. Vanberghem ◽  
...  
Keyword(s):  
G Protein ◽  
Olfactory Receptor ◽  
Large Scale ◽  
Scale Production ◽  
G Protein Coupled Receptor ◽  
Large Scale Production ◽  
G Protein Coupled

Mammalian G-protein-coupled receptor expression in Escherichia coli: I. High-throughput large-scale production as inclusion bodies

2009 ◽  
Vol 386 (2) ◽  
pp. 147-155 ◽  
Author(s):  
Kerstin Michalke ◽  
Marie-Eve Gravière ◽  
Céline Huyghe ◽  
Renaud Vincentelli ◽  
Renaud Wagner ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
G Protein ◽  
High Throughput ◽  
Inclusion Bodies ◽  
Large Scale ◽  
Receptor Expression ◽  
Scale Production ◽  
Expression In Escherichia Coli ◽  
Large Scale Production ◽  
G Protein Coupled

Some effects of putative G-protein biased mu-opioid receptor agonists in male rhesus monkeys

2021 ◽  
Vol Publish Ahead of Print ◽  
Author(s):  
Jeremy C. Cornelissen ◽  
Bruce E. Blough ◽  
Laura M. Bohn ◽  
S. Stevens Negus ◽  
Matthew L. Banks
Keyword(s):  
G Protein ◽  
Opioid Receptor ◽  
Rhesus Monkeys ◽  
Mu Opioid Receptor ◽  
Mu Opioid ◽  
Receptor Agonists ◽  
Opioid Receptor Agonists ◽  
Male Rhesus
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