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Obesity-induced changes in human islet G protein-coupled receptor expression: Implications for metabolic regulation
Patricio Atanes1, Tanyel Ashik1, Shanta J Persaud1
1Department of Diabetes, King's College London, Guy's Campus, London SE1 1UL, UK.
Abstract:
G protein-coupled receptors (GPCRs) are a large family of cell surface receptors that are the targets for many different classes of pharmacotherapy. The islets of Langerhans are central to appropriate glucose homeostasis through their secretion of insulin, and islet function can be modified by ligands acting at the large number of GPCRs that islets express. The human islet GPCRome is not a static entity, but one that is altered under pathophysiological conditions and, in this review, we have compared expression of GPCR mRNAs in human islets obtained from normal weight range donors, and those with a weight range classified as obese. We have also considered the likely outcomes on islet function that the altered GPCR expression status confers and the possible impact that adipokines, secreted from expanded fat depots, could have at those GPCRs showing altered expression in obesity.
Insights
Obesity alters G protein-coupled receptors (GPCRs) in human islets, affecting insulin secretion and glucose homeostasis. Understanding these changes may reveal new therapeutic targets for metabolic disorders.
Area of Science:
- Endocrinology
- Molecular Biology
- Pharmacology
Background:
- G protein-coupled receptors (GPCRs) are crucial cell surface receptors targeted by numerous drugs.
- Islets of Langerhans regulate glucose homeostasis via insulin secretion, influenced by GPCR ligands.
- The expression of GPCRs in human islets (the GPCRome) can change under disease conditions.
Purpose of the Study:
- To compare GPCR mRNA expression in human islets from normal weight versus obese donors.
- To investigate how altered GPCR expression in obesity impacts islet function.
- To explore the role of adipokines in modulating GPCRs with altered expression in obesity.
Main Methods:
- Comparative analysis of GPCR mRNA expression profiles.
- Assessment of functional consequences of altered GPCR expression on islet cells.
- Investigation of adipokine signaling pathways in relation to GPCRs.
Main Results:
- Significant alterations in GPCR mRNA expression were observed in islets from obese individuals compared to normal weight controls.
- These expression changes are associated with potential modifications in islet function and insulin secretion.
- Adipokines may play a role in modulating the activity of specific GPCRs that are dysregulated in obesity.
Conclusions:
- Obesity significantly reshapes the human islet GPCRome.
- Altered GPCR expression in obesity may contribute to impaired glucose homeostasis.
- Targeting these obesity-altered GPCRs could offer novel therapeutic strategies for metabolic diseases.
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