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Adhesion G protein-coupled receptors (GPCRs) are implicated in numerous human diseases. However, to date, no medicinal product has been approved that specifically targets these signalling molecules. Researchers at Leipzig University and Shandong University have summarised the therapeutic potential of these receptors in a high-profile study. At present, 17 of the 33 known human adhesion GPCRs are associated with specific diseases. This opens up a broad range of targets for the development of novel medicinal products. The work has been published in Nature Reviews Drug Discovery, one of the world’s leading journals in this field.
Adhesion GPCRs are a large class of surface proteins that recognise chemical and mechanical stimuli in the body. The rapidly expanding body of knowledge on the therapeutic targeting of these receptors is raising hopes for clinical application in the near future. Although no medicinal products targeting these receptors have yet been approved, several adhesion GPCR modulators are available and show potential for translation into clinical use. Modulators are crucial for the regulation of metabolic pathways and play a major role in pharmacology by enabling the targeted control of receptor activity.
The new study provides a comprehensive compilation of all known natural and synthetic therapeutic modulators of adhesion GPCRs, evaluates how they work, and presents key data on effective concentrations in clearly structured tables. It also offers an overview of the physiological functions of this receptor family identified to date. The scholarly article condenses 30 years of research on adhesion GPCRs into nearly 300 references, tracing the path from molecules with previously unknown functions to tangible therapeutic strategies. The information is intended to serve as practical guidance for researchers, clinicians and representatives of the pharmaceutical industry. “Knowledge about the role of adhesion GPCRs in human disease is expanding rapidly. With our work, we aim to help further strengthen the bridge between basic research and clinical application,” says Professor Ines Liebscher, study lead at the Rudolf Schönheimer Institute of Biochemistry, part of the Faculty of Medicine.
Researchers at the institute are currently developing new compounds designed to target individual signalling pathways of these receptors. Particular attention is being paid to what are called biased agonists – active substances that selectively stimulate specific signalling cascades and may therefore minimise unwanted side effects. In addition to their influence on metabolic processes, diseases of the cardiovascular system, myelination disorders and cancer development are also a focus of research.
Researchers at Leipzig University and Shandong University only recently jointly discovered the active compound AP503, a highly specific activator of the adhesion GPCR GPR133. In various mouse models, AP503 was shown to improve muscle contractility and to mitigate bone loss associated with osteoporosis. The article in Nature Reviews Drug Discovery marks the fourth successful collaboration between the Rudolf Schönheimer Institute of Biochemistry and the team led by Professor Jin-Peng Sun at Shandong University. Publishing a review article in this renowned journal – which contextualises major advances in therapeutic research and informs future research priorities – is considered a significant distinction, as articles are accepted by invitation only.
Further information: For more than ten years, adhesion G protein-coupled receptors have been a major research focus at Leipzig University. Since 2019, researchers have also been working on this topic within Collaborative Research Centre 1423: Structural Dynamics of GPCR Activation and Signaling. Internationally, Leipzig is regarded as a leading centre in this field of research.
Translation: Matthew Rockey
Professor Ines Liebscher
Rudolf Schönheimer Institute of Biochemistry
Faculty of Medicine, Leipzig University
Email: Ines.liebscher@medizin.uni-leipzig.de
Tel.: +49341/97-22141
Original publication in Nature Reviews Drug Discovery: The therapeutic potential of orphan adhesion G-protein-coupled receptors. DOI: https://doi.org/10.1038/s41573-025-01371-6
https://www.uni-leipzig.de/newsdetail/artikel/forschung-fuer-staerkere-knochen-u...
Modulators play a major role in the targeted control of receptor activity. Several modulators of adh ...
Source: graphic created with Illustrae
Copyright: Ines Liebscher
Professor Ines Liebscher
Source: private
Copyright: Leipzig University
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