Key result
Pharmacologically targeting G protein-coupled receptors on brown and beige adipocytes represents a promising but challenging therapeutic strategy for counteracting obesity and diabetes.
Why the study?
Engaging the energy-dissipating activities of thermogenic brown and beige adipocytes has gained attention as a therapeutic strategy for metabolic diseases, prompting the need to review advances, opportunities, and challenges in targeting GPCR signaling.
Targeting GPCR signaling in thermogenic fat is a promising but challenging therapeutic strategy for counteracting metabolic diseases like obesity and diabetes.
Thermogenic adipocyte targeting may confer cardiometabolic protection; leaves open clinical translation pending interventional human data.
BACKGROUND: Thermogenic brown and beige adipocytes are recognized for their unique capacity to consume extraordinary levels of metabolites and lipids from the blood to fuel heat-producing catabolic processes [1-7]. In humans, the functions of thermogenic adipocytes are associated with cardiometabolic protection and improved glycemic control [8-13]. Consequently, engaging these macronutrient-consuming and energy-dissipating activities has gained attention as a promising therapeutic strategy for counteracting metabolic diseases, such as obesity and diabetes. SCOPE OF REVIEW: In this review, we highlight new advances in our understanding of the physiological role of G protein-coupled receptors (GPCRs) in controlling thermogenic adipocyte biology. We further extend our discussion to the opportunities and challenges posed by pharmacologically targeting different elements of GPCR signaling in these highly specialized fat cells. MAJOR CONCLUSIONS: 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. Therefore, continued interrogation across the GPCR landscape is necessary for future leaps within the field of thermogenic fat biology to unlock the therapeutic potential of adipocyte catabolism.
No takes yet. Share an insight, caveat, or question.
Johansen et al. (2022) conducted a review in Metabolic diseases (obesity and diabetes). Pharmacologically targeting GPCR signaling in thermogenic fat was evaluated. Pharmacologically targeting G protein-coupled receptors on brown and beige adipocytes represents a promising but challenging therapeutic strategy for counteracting obesity and diabetes.
Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context: