Hormonal
Pharmacological activation of G protein-coupled receptors (GPCRs) in thermogenic brown and beige adipocytes can increase energy expenditure and improve metabolic health, but current adrenergic agonists have a narrow safety window due to cardiovascular side effects.
While cold exposure is a natural way to activate brown fat, scientists are developing drugs that target specific receptors (GPCRs) to do the same thing. Current drugs like mirabegron show promise for boosting metabolism by ~200 kcal/day, but they can affect heart rate. Future treatments aim to target these receptors more selectively to avoid side effects while still improving metabolic health.
GPCRs represent appealing candidates through which to harness adipose thermogenesis. Yet safely and effectively targeting these druggable receptors on brown and beige adipocytes has thus far proven challenging.
Why this rating
Based on a comprehensive review of multiple clinical and preclinical studies.
Source
Leveraging GPCR signaling in thermogenic fat to counteract metabolic diseases
Olivia Sveidahl Johansen et al. · Molecular Metabolism · 2022
DOI 10.1016/j.molmet.2022.101474
More from this paper
- Non-adrenergic Gs-coupled receptors (e.g., secretin, glucagon, adenosine) can stimulate brown adipose tissue thermogenesis independently of the sympathetic nervous system, offering a potential pathway to avoid cardiovascular side effects associated with adrenergic agonists.Good
- Activation of Gq-coupled receptors in brown and beige adipocytes generally suppresses thermogenic competence, whereas specific Gq receptors (like GPR120) can boost lipid oxidation and mitochondrial respiration.Moderate
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