scholarly journals Myricetin: a potent approach for the treatment of type 2 diabetes as a natural class B GPCR agonist

2017 ◽  
Vol 31 (6) ◽  
pp. 2603-2611 ◽  
Author(s):  
Ying Li ◽  
Xuemin Zheng ◽  
Xiulin Yi ◽  
Changxiao Liu ◽  
Dexin Kong ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Natural Class ◽  
Class B ◽  
Class B Gpcr

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 Expression Levels and Genetic Polymorphism of Scavenger Receptor Class B Type 1 as a Biomarker of Type 2 Diabetes Mellitus

2021 ◽  
Author(s):  
Mohd Wamique ◽  
D. Himanshu ◽  
Wahid Ali
Keyword(s):  
Diabetes Mellitus ◽  
Type 2 Diabetes ◽  
Type 2 Diabetes Mellitus ◽  
Genetic Polymorphism ◽  
Western Blot ◽  
Scavenger Receptor ◽  
Scavenger Receptor Class ◽  
Class B

Objectives: The present study aimed to determine whether the expression level and genetic polymorphism scavenger receptor class B type 1 (SRB1) rs5888 may be used as biological markers in type 2 diabetes mellitus (T2DM). Methods: A total of 600 individuals, including 300 T2DM and 300 healthy individuals, were enrolled in the study from April 2016 to April 2017. Blood samples were collected from each T2DM and healthy individual. Total proteins were determined using western blot analysis. Also, restriction fragment length polymor­phism (RFLP) analysis was achieved to detect the incidence of genetic polymorphisms. Results: Western blot analysis results revealed that the protein expression of SRB1 was significantly decreased in T2DM of SRB1 CC variant as compared with controls. The genotype distribution and the allelic frequencies for the SRB1 polymorphism were significantly different than T2DM and controls. CC genotype of the SRB1 polymorphism showed a potential association with the incidence of T2DM (OR =1.19, 95% CI 0.63 - 2.25, P=0.577). Conclusions: The expression levels and genetic polymorphisms of SRB1 CC variant may be potential biomarkers for the occurrence of T2DM. Keywords: Polymorphism; T2DM; SRB1, Protein expression; Biomarker

scholarly journals Hyperglycemia promotes overexpression of SR-BII isoform of the scavenger receptor class B type I in type 2 diabetes mellitus: A study in Juana Koslay City, San Luis, Argentina

2013 ◽  
Vol 03 (04) ◽  
pp. 172-183
Author(s):  
Gisela V. Mendoza ◽  
Susana Siewert ◽  
Irma González ◽  
María C. Della Vedova ◽  
Gustavo Fernandez ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Type 2 Diabetes ◽  
Type 2 Diabetes Mellitus ◽  
Scavenger Receptor ◽  
Type I ◽  
San Luis ◽  
Scavenger Receptor Class ◽  
Class B

The complexity of signalling mediated by the glucagon-like peptide-1 receptor

2016 ◽  
Vol 44 (2) ◽  
pp. 582-588 ◽  
Author(s):  
Madeleine M. Fletcher ◽  
Michelle L. Halls ◽  
Arthur Christopoulos ◽  
Patrick M. Sexton ◽  
Denise Wootten
Keyword(s):  
Type 2 Diabetes ◽  
Cell Mass ◽  
Peripheral Tissues ◽  
Biased Agonism ◽  
Temporal Aspects ◽  
Class B ◽  
Future Drug ◽  
Glucagon Like Peptide ◽  
Glucagon Like Peptide 1

The glucagon-like peptide-1 receptor (GLP-1R) is a class B GPCR that is a major therapeutic target for the treatment of type 2 diabetes. The receptor is activated by the incretin peptide GLP-1 promoting a broad range of physiological effects including glucose-dependent insulin secretion and biosynthesis, improved insulin sensitivity of peripheral tissues, preservation of β-cell mass and weight loss, all of which are beneficial in the treatment of type 2 diabetes. Despite this, existing knowledge surrounding the underlying signalling mechanisms responsible for the physiological actions downstream of GLP-1R activation is limited. Here, we review the current understanding around GLP-1R-mediated signalling, in particular highlighting recent contributions to the field on biased agonism, the spatial and temporal aspects for the control of signalling and how these concepts may influence future drug development.

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