The relevance of adhesion G protein-coupled receptors in metabolic functions
- PMID: 34218541
- DOI: 10.1515/hsz-2021-0146
The relevance of adhesion G protein-coupled receptors in metabolic functions
Abstract
G protein-coupled receptors (GPCRs) modulate a variety of physiological functions and have been proven to be outstanding drug targets. However, approximately one-third of all non-olfactory GPCRs are still orphans in respect to their signal transduction and physiological functions. Receptors of the class of Adhesion GPCRs (aGPCRs) are among these orphan receptors. They are characterized by unique features in their structure and tissue-specific expression, which yields them interesting candidates for deorphanization and testing as potential therapeutic targets. Capable of G-protein coupling and non-G protein-mediated function, aGPCRs may extend our repertoire of influencing physiological function. Besides their described significance in the immune and central nervous systems, growing evidence indicates a high importance of these receptors in metabolic tissue. RNAseq analyses revealed high expression of several aGPCRs in pancreatic islets, adipose tissue, liver, and intestine but also in neurons governing food intake. In this review, we focus on aGPCRs and their function in regulating metabolic pathways. Based on current knowledge, this receptor class represents high potential for future pharmacological approaches addressing obesity and other metabolic diseases.
Keywords: aGPCR; adipose tissue; metabolism; pancreatic islet.
© 2021 Isabell Kaczmarek et al., published by De Gruyter, Berlin/Boston.
References
-
- Ackerman, S.D., Luo, R., Poitelon, Y., Mogha, A., Harty, B.L., D’Rozario, M., Sanchez, N.E., Lakkaraju, A.K.K., Gamble, P., Li, J., et al. (2018). GPR56/ADGRG1 regulates development and maintenance of peripheral myelin. J. Exp. Med. 215: 941–961, https://doi.org/10.1084/jem.20161714.
-
- Adan, R.A.H., Tiesjema, B., Hillebrand, J.J.G., La Fleur, S.E., Kas, M.J.H., and de Krom, M. (2006). The MC4 receptor and control of appetite. Br. J. Pharmacol. 149: 815–827, https://doi.org/10.1038/sj.bjp.0706929.
-
- Adriaenssens, A.E., Svendsen, B., Lam, B.Y.H., Yeo, G.S.H., Holst, J.J., Reimann, F., and Gribble, F.M. (2016). Transcriptomic profiling of pancreatic alpha, beta and delta cell populations identifies delta cells as a principal target for ghrelin in mouse islets. Diabetologia 59: 2156–2165, https://doi.org/10.1007/s00125-016-4033-1.
-
- Ahrén, B. (2009). Islet G protein-coupled receptors as potential targets for treatment of type 2 diabetes. Nat. Rev. Drug Discov. 8: 369–385, https://doi.org/10.1038/nrd2782.
-
- Al Hasan, M., Roy, P., Dolan, S., Martin, P.E., Patterson, S., and Bartholomew, C. (2020). Adhesion G-protein coupled receptor 56 is required for 3T3-L1 adipogenesis. J. Cell. Physiol. 235: 1601–1614, https://doi.org/10.1002/jcp.29079.
Publication types
MeSH terms
Substances
LinkOut - more resources
Full Text Sources