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Institute of Pharmacy, Pharmaceutical/Medicinal Chemistry & Tübingen Center for Academic Drug Discovery (TüCAD2) Eberhard Karls University Tübingen, Auf der Morgenstelle 8, 72076 Tübingen, Germany

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Julien Hanson

https://orcid.org/0000-0001-7063-7590

Laboratory of Molecular Pharmacology, GIGA-Molecular Biology of Diseases, University of Liège, B-4000 Liège, Belgium

Laboratory of Medicinal Chemistry, Centre for Interdisciplinary Research on Medicines (CIRM), University of Liège, B-4000 Liège, Belgium

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Stefan Laufer

https://orcid.org/0000-0001-6952-1486

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Thanigaimalai Pillaiyar

*Author for correspondence: Tel.: +49 707 1297 7458;

E-mail Address: thanigaimalai.pillaiyar@uni-tuebingen.de

https://orcid.org/0000-0001-5575-8896

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Published Online:10 May 2022https://doi.org/10.4155/fmc-2022-0006

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Abstract

The super-conserved receptors expressed in the brain (SREB) constitute a family of orphan G protein-coupled receptors that include GPR27 (SREB1), GPR85 (SREB2) and GPR173 (SREB3). Their sequences are highly conserved in vertebrates, and they are almost exclusively expressed in the central nervous system. This family of receptors has attracted much attention due to their putative physiological functions and their potential as novel drug targets. The SREB family has been postulated to play important roles in a wide range of different diseases, including pancreatic β-cell insulin secretion and regulation, schizophrenia, autism and atherosclerosis. This review intends to provide a comprehensive overview of the SREB family and its recent advances in biology and medicinal chemistry.

Plain language summary

In recent years, the super-conserved receptors expressed in the brain called GPR27, GPR85 and GPR173 have attracted much interest in the field of medicinal science. They have one important feature in common: they are all almost entirely found in the brain. Researchers have investigated their functions in the body in various animal models, as well as their utility in future drug development. GPR27 has been found to be involved in insulin and blood sugar processes in the body and therefore may be important for diabetes treatment. GPR85 is thought to be linked to brain diseases such as schizophrenia and autism. GPR173 is linked to many different illnesses, including atherosclerosis (the buildup of fats, cholesterol and other substances in arteries) and Type 2 diabetes.

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Papers of special note have been highlighted as: • of interest

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Vol. 14, No. 12

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Received 11 January 2022

Accepted 22 April 2022

Published online 10 May 2022

Published in print June 2022

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Acknowledgments

The authors thank K Schmidt for proofreading (language). TüCAD2 is funded by the Federal Ministry of Education and Research (BMBF) and the Baden-Württemberg Ministry of Science as part of the Excellence Strategy of the German Federal and State Governments. J Hanson is an F.R.S.-FNRS senior research associate and was supported by a research project grant from the F.R.S.-FNRS (PDRT.0111.19).

Financial & competing interests disclosure

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending or royalties.

No writing assistance was utilized in the production of this manuscript.

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Super-conserved receptors expressed in the brain: biology and medicinal chemistry efforts

Abstract

Plain language summary

References