Islet G protein-coupled receptors as potential targets for treatment of type 2 diabetes

2009 ◽  
Vol 8 (5) ◽  
pp. 369-385 ◽  
Author(s):  
Bo Ahrén
Keyword(s):  
Type 2 Diabetes ◽  
G Protein ◽  
G Protein Coupled Receptors ◽  
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 Targeting islet G-protein-coupled receptors for type 2 diabetes therapy

2021 ◽  
Author(s):  
Shanta J. Persaud ◽  
Oladapo E. Olaniru ◽  
Patricio Atanes
Keyword(s):  
Type 2 Diabetes ◽  
G Protein ◽  
G Protein Coupled Receptors ◽  
Pharmaceutical Companies ◽  
Β Cells ◽  
Diabetes Therapy ◽  
Wide Range ◽  
Mass Expansion ◽  
G Protein Coupled

The majority of people with diabetes have type 2 diabetes (T2D), where hyperglycaemia occurs because the islet β-cells are unable to secrete enough insulin, usually in the context of insulin resistance that arises because of fat mass expansion. There are a range of pharmacotherapies in current use to treat T2D and pharmaceutical companies are actively engaged in the development of novel therapies for better glucose control. Ligands that target G-protein-coupled receptors (GPCRs) are obvious candidates because they are used successfully for a wide range of disorders and GLP-1 receptor agonists, which are a relatively recent class of diabetes therapy, have proved to be very effective in treating T2D. We provide here an overview of current successes, some drawbacks and future possibilities for GPCR-based T2D therapies.

scholarly journals Metabolic Functions of G Protein-Coupled Receptors and β-Arrestin-Mediated Signaling Pathways in the Pathophysiology of Type 2 Diabetes and Obesity

2021 ◽  
Vol 12 ◽  
Author(s):  
Camila Oliveira de Souza ◽  
Xuenan Sun ◽  
Dayoung Oh
Keyword(s):  
Type 2 Diabetes ◽  
Signaling Pathways ◽  
G Protein ◽  
Metabolic Disorders ◽  
G Protein Coupled Receptors ◽  
Transmembrane Receptors ◽  
Therapeutic Drugs ◽  
Metabolic Functions ◽  
G Protein Coupled

Seven transmembrane receptors (7TMRs), often termed G protein-coupled receptors (GPCRs), are the most common target of therapeutic drugs used today. Many studies suggest that distinct members of the GPCR superfamily represent potential targets for the treatment of various metabolic disorders including obesity and type 2 diabetes (T2D). GPCRs typically activate different classes of heterotrimeric G proteins, which can be subgrouped into four major functional types: Gαs, Gαi, Gαq/11, and G12/13, in response to agonist binding. Accumulating evidence suggests that GPCRs can also initiate β-arrestin-dependent, G protein-independent signaling. Thus, the physiological outcome of activating a certain GPCR in a particular tissue may also be modulated by β-arrestin-dependent, but G protein-independent signaling pathways. In this review, we will focus on the role of G protein- and β-arrestin-dependent signaling pathways in the development of obesity and T2D-related metabolic disorders.

scholarly journals Sera from Patients with Type 2 Diabetes Contain Agonistic Autoantibodies Against G Protein-Coupled Receptors

2009 ◽  
Vol 70 (2) ◽  
pp. 159-160 ◽  
Author(s):  
P. Hempel ◽  
P. Karczewski ◽  
K.-D. Kohnert ◽  
J. Raabe ◽  
B. Lemke ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
G Protein ◽  
G Protein Coupled Receptors ◽  
Agonistic Autoantibodies ◽  
G Protein Coupled

scholarly journals G Protein–Coupled Receptors Targeting Insulin Resistance, Obesity, and Type 2 Diabetes Mellitus

2017 ◽  
Vol 70 (1) ◽  
pp. 39-67 ◽  
Author(s):  
Darren M. Riddy ◽  
Philippe Delerive ◽  
Roger J. Summers ◽  
Patrick M. Sexton ◽  
Christopher J. Langmead
Keyword(s):  
Diabetes Mellitus ◽  
Insulin Resistance ◽  
Type 2 Diabetes ◽  
Type 2 Diabetes Mellitus ◽  
G Protein ◽  
G Protein Coupled Receptors ◽  
G Protein Coupled
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