scholarly journals Spirohexene-Tetrazine Ligation Enables Bioorthogonal Labeling of Class B G Protein-Coupled Receptors in Live Cells

2017 ◽  
Vol 139 (38) ◽  
pp. 13376-13386 ◽  
Author(s):  
Carlo P. Ramil ◽  
Maoqing Dong ◽  
Peng An ◽  
Tracey M. Lewandowski ◽  
Zhipeng Yu ◽  
...  
Keyword(s):  
G Protein ◽  
G Protein Coupled Receptors ◽  
Live Cells ◽  
Bioorthogonal Labeling ◽  
Class B ◽  
G Protein Coupled ◽  
Tetrazine Ligation

Quantitative Single-Residue Bioorthogonal Labeling of G Protein-Coupled Receptors in Live Cells

2019 ◽  
Vol 14 (6) ◽  
pp. 1141-1149 ◽  
Author(s):  
Robert Serfling ◽  
Lisa Seidel ◽  
Andreas Bock ◽  
Martin J. Lohse ◽  
Paolo Annibale ◽  
...  
Keyword(s):  
G Protein ◽  
G Protein Coupled Receptors ◽  
Live Cells ◽  
Bioorthogonal Labeling ◽  
G Protein Coupled

scholarly journals Mini G protein probes for active G protein–coupled receptors (GPCRs) in live cells

2018 ◽  
Vol 293 (19) ◽  
pp. 7466-7473 ◽  
Author(s):  
Qingwen Wan ◽  
Najeah Okashah ◽  
Asuka Inoue ◽  
Rony Nehmé ◽  
Byron Carpenter ◽  
...  
Keyword(s):  
G Protein ◽  
G Protein Coupled Receptors ◽  
Live Cells ◽  
G Protein Coupled

scholarly journals Structure and mechanism for recognition of peptide hormones by Class B G-protein-coupled receptors

2012 ◽  
Vol 33 (3) ◽  
pp. 300-311 ◽  
Author(s):  
Kuntal Pal ◽  
Karsten Melcher ◽  
H Eric Xu
Keyword(s):  
G Protein ◽  
Peptide Hormones ◽  
G Protein Coupled Receptors ◽  
Class B ◽  
G Protein Coupled

scholarly journals Interaction of Glucagon G-Protein Coupled Receptor with Known Natural Antidiabetic Compounds: MultiscoringIn SilicoApproach

2015 ◽  
Vol 2015 ◽  
pp. 1-6 ◽  
Author(s):  
M. H. Baig ◽  
K. Ahmad ◽  
Q. Hasan ◽  
M. K. A. Khan ◽  
N. S. Rao ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
G Protein ◽  
Scoring Function ◽  
Natural Compounds ◽  
G Protein Coupled Receptors ◽  
Binding Potential ◽  
Glucagon Receptor ◽  
Class B ◽  
G Protein Coupled

Glucagon receptor (GCGR) is a secretin-like (class B) family of G-protein coupled receptors (GPCRs) in humans that plays an important role in elevating the glucose concentration in blood and has thus become one of the promising therapeutic targets for treatment of type 2 diabetes mellitus. GCGR based inhibitors for the treatment of type 2 diabetes are either glucagon neutralizers or small molecular antagonists. Management of diabetes without any side effects is still a challenge to the medical system, and the search for a new and effective natural GCGR antagonist is an important area for the treatment of type 2 diabetes. In the present study, a number of natural compounds containing antidiabetic properties were selected from the literature and their binding potential against GCGR was determined using molecular docking and otherin silicoapproaches. Among all selected natural compounds, curcumin was found to be the most effective compound against GCGR followed by amorfrutin 1 and 4-hydroxyderricin. These compounds were rescored to confirm the accuracy of binding using another scoring function (x-score). The final conclusions were drawn based on the results obtained from the GOLD andx-score. Further experiments were conducted to identify the atomic level interactions of selected compounds with GCGR.

scholarly journals Structural Basis for Allosteric Modulation of Class B G Protein–Coupled Receptors

2020 ◽  
Vol 60 (1) ◽  
pp. 89-107 ◽  
Author(s):  
Denise Wootten ◽  
Laurence J. Miller
Keyword(s):  
G Protein ◽  
Allosteric Modulation ◽  
G Protein Coupled Receptors ◽  
Structural Basis ◽  
Allosteric Modulators ◽  
Class B ◽  
Endogenous Proteins ◽  
And Function ◽  
Agonist Ligands ◽  
G Protein Coupled

Recent advances in our understanding of the structure and function of class B G protein–coupled receptors (GPCRs) provide multiple opportunities for targeted development of allosteric modulators. Given the pleiotropic signaling patterns emanating from these receptors in response to a variety of natural agonist ligands, modulators have the potential to sculpt the responses to meet distinct needs of different groups of patients. In this review, we provide insights into how this family of GPCRs differs from the rest of the superfamily, how orthosteric agonists bind and activate these receptors, the potential for allosteric modulators to interact with various regions of these targets, and the allosteric influence of endogenous proteins on the pharmacology of these receptors, all of which are important considerations when developing new therapies.

Sign in / Sign up

Export Citation Format

Share Document