Split-Tobacco Etch Virus (Split-TEV) Method in G Protein-Coupled Receptor Interacting Proteins

Author(s):  
Marta Alonso-Gardón ◽  
Raúl Estévez
2021 ◽  
Vol 12 ◽  
Author(s):  
Seunghun P. Lee ◽  
Jenson Qi ◽  
Guozhang Xu ◽  
Matthew M. Rankin ◽  
James Littrell ◽  
...  

The glucagon-like peptide-1 receptor (GLP-1R) is a G-protein-coupled receptor (GPCR) whose activation results in suppression of food intake and improvement of glucose metabolism. Several receptor interacting proteins regulate the signaling of GLP-1R such as G protein-coupled receptor kinases (GRK) and β-arrestins. Here we evaluated the physiological and pharmacological impact of GRK inhibition on GLP-1R activity leveraging small molecule inhibitors of GRK2 and GRK3. We demonstrated that inhibition of GRK: i) inhibited GLP-1-mediated β-arrestin recruitment, ii) enhanced GLP-1-induced insulin secretion in isolated islets and iii) has additive effect with dipeptidyl peptidase 4 in mediating suppression of glucose excursion in mice. These findings highlight the importance of GRK to modulate GLP-1R function in vitro and in vivo. GRK inhibition is a potential therapeutic approach to enhance endogenous and pharmacologically stimulated GLP-1R signaling.


2004 ◽  
Vol 32 (5) ◽  
pp. 878-880 ◽  
Author(s):  
G. Milligan ◽  
H. Murdoch ◽  
E. Kellett ◽  
J.H. White ◽  
G.-J. Feng

A substantial number of G-protein-coupled receptor-interacting proteins have been identified initially by the use of yeast two-hybrid screens. Using the C-terminal tail of both opioid receptors and the melanin concentrating hormone receptor-1 as bait, the actin and intermediate filament-binding protein periplakin was isolated. In each case, the site of interaction is within helix VIII of the receptor and periplakin limits agonist-mediated G-protein activation potentially by competing with G-protein for this region of the receptor.


2011 ◽  
Vol 412 (2) ◽  
pp. 141-152 ◽  
Author(s):  
Minou S. Djannatian ◽  
Sabrina Galinski ◽  
Tobias M. Fischer ◽  
Moritz J. Rossner

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