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Recently, due to dietary and lifestyle factors, the prevalence of obesity and closely associated metabolic disorders has been steadily increasing in developed affluent countries. This is a major public-health challenge which has attracted intense interest from the biopharmaceutical industry. There are several members of the GPCR superfamily that are potential targets for treating obesity and its closely associated spectrum of metabolic disorders.
The regulation of energy metabolism requires the well-balanced control of opposing metabolic pathways — such as lipogenesis and lipolysis, glycolysis and gluconeogenesis, or fatty acid oxidation and synthesis — which is often disturbed in metabolic diseases such as type 2 diabetes, obesity and dyslipidemia. Given their key role in the coordination of metabolic processes, metabolite-sensing GPCRs are possible targets for drugs that modulate metabolic fluxes and consequently influence the outcome of metabolic disorders. For instance, metabolite-sensing GPCRs that are highly expressed by adipocytes can be targeted to regulate lipolytic activity, with the aim of lowering plasma lipid levels or lipid storage in the treatment of obesity or dyslipidemia. Other GPCRs expressed by enteroendocrine cells or in insulin-producing pancreatic β-cells may be targeted to control insulin production and release in the treatment of diabetes. Moreover, several metabolite-sensing GPCRs are expressed by immune cells, thus providing a link between the metabolic system and the immune system, which may be exploited pharmacologically to influence inflammatory processes involved in metabolic diseases.
The current molecular biology toolkit for GPCRs has powered drug discovery research toward the generation of some investigational molecules for treating metabolic diseases, and there is a wealth of publications and clinical trials that exemplify this. Creative Biogene can offer a variety of GPCR related products including stable cell lines, viral particles and clones for your drug discovery projects in metabolic disorders.
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