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Annual Review of Pharmacology and Toxicology

Volume 61, 2021

Use of DREADD Technology to Identify Novel Targets for Antidiabetic Drugs

Abstract

G protein–coupled receptors (GPCRs) form a superfamily of plasma membrane receptors that couple to four major families of heterotrimeric G proteins, G, G, G, and G. GPCRs represent excellent targets for drug therapy. Since the individual GPCRs are expressed by many different cell types, the in vivo metabolic roles of a specific GPCR expressed by a distinct cell type are not well understood. The development of designer GPCRs known as DREADDs (designer receptors exclusively activated by a designer drug) that selectively couple to distinct classes of heterotrimeric G proteins has greatly facilitated studies in this area. This review focuses on the use of DREADD technology to explore the physiological and pathophysiological roles of distinct GPCR/G protein cascades in several metabolically important cell types. The novel insights gained from these studies should stimulate the development of GPCR-based treatments for major metabolic diseases such as type 2 diabetes and obesity.

Keyword(s): DREADD technology, G proteins, G protein–coupled receptors, mutant mouse models, obesity, type 2 diabetes
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2021-01-06
2025-04-21
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Use of DREADD Technology to Identify Novel Targets for Antidiabetic Drugs
Annual Review of Pharmacology and Toxicology 61, 421 (2021); https://doi.org/10.1146/annurev-pharmtox-030220-121042
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  • Article Type: Review Article

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