A potential role for GPR55 in the regulation of energy homeostasis

• Published in: Drug discovery today 2014-08, Vol.19 (8), p.1145-1151
• Main Authors: Simcocks, Anna C., O’Keefe, Lannie, Jenkin, Kayte A., Mathai, Michael L., Hryciw, Deanne H., McAinch, Andrew J.
• Format: Article
• Language: English
• Subjects: Animals; Diabetes Mellitus, Type 2 - metabolism; Energy Metabolism - physiology; Homeostasis - physiology; Humans; Receptors, G-Protein-Coupled - metabolism
• ISSN: 1359-6446; 1878-5832
• DOI: 10.1016/j.drudis.2013.12.005

•GPR55 is a putative cannabinoid receptor.•It is expressed in tissues involved in regulating energy intake and expenditure, expression in brown fat is however unknown.•There is limited research into the role of GPR55 in the obese state.•Research into newly developed second generation selective GPR55 agonists and antagonists is preliminary.•Future research into their role on tissues involved in regulating energy intake and expenditure is warranted. G protein-coupled receptor 55 (GPR55) is a putative cannabinoid receptor that is expressed in several tissues involved in regulating energy homeostasis, including the hypothalamus, gastrointestinal tract, pancreas, liver, white adipose and skeletal muscle. GPR55 has been shown to have a role in cancer and gastrointestinal inflammation, as well as in obesity and type 2 diabetes mellitus (T2DM). Despite this, the (patho)physiological role of GPR55 in cell dysfunction is still poorly understood, largely because of the limited identification of downstream signalling targets. Nonetheless, research has suggested that GPR55 modulation would be a useful pharmacological target in metabolically active tissues to improve treatment of diseases such as obesity and T2DM. Further research is essential to gain a better understanding of the role that this receptor might have in these and other pathophysiological conditions.