Abstract
The internalization of G protein-coupled receptors (GPCRs) is an important mechanism regulating the signal strength and limiting the opportunity of receptor activation. Based on the importance of GPCRs, the detailed knowledge about the regulation of signal transduction is crucial. Here, current knowledge about the agonist-induced, arrestin-dependent internalization process of rhodopsin-like GPCRs is reviewed. Arrestins are conserved molecules that act as key players within the internalization process of many GPCRs. Based on highly conserved structural characteristics within the rhodopsin-like GPCRs, the identification of arrestin interaction sites in model systems can be compared and used for the investigation of internalization processes of other receptors. The increasing understanding of this essential regulation mechanism of receptors can be used for drug development targeting rhodopsin-like GPCRs. Here, we focus on the neuropeptide Y receptor family, as these receptors transmit various physiological processes such as food intake, energy homeostasis, and regulation of emotional behavior, and are further involved in pathophysiological processes like cancer, obesity and mood disorders. Hence, this receptor family represents an interesting target for the development of novel therapeutics requiring the understanding of the regulatory mechanisms influencing receptor mediated signaling.
Funding source: Deutsche Forschungsgemeinschaft
Award Identifier / Grant number: 421152132, SFB 1423, A04/B01
About the authors
Lizzy Wanka studied biochemistry, bachelor and master, at Leipzig University. She performed her PhD studies in Leipzig in the lab of Prof. Dr. Annette G. Beck-Sickinger about the Arrestin-3 recruitment of human neuropeptid Y receptors. Currently, she is working in the research center Borstel in the working group clinical and molecular allergology of Prof. Dr. Uta Jappe investigating allergens and their molecular impact on cells.
Victoria Behr earned her bachelor’s and master’s degree in biochemistry from the Leipzig University (Leipzig, Germany), broadening the scope of her studies with an internship at NSTDA-BIOTEC (Thailand). She is now doing her PhD in Professor Annette G. Beck-Sickinger’s group at the Leipzig University, focusing on the investigation of G protein-coupled receptors by performing cell-based assays and protein expression.
Annette G. Beck-Sickinger is professor of biochemistry and bioorganic chemistry at Leipzig University (Germany). Her major research fields include structure-activity relationships of peptide/protein hormones and G protein-coupled receptors. She has been awarded many prizes including the Leonidas Zervas Award of the European Peptide Society, the gold medal of the Max-Bergmann-Kreis (2009), the Albrecht Kossel Award of Biochemistry of the GDCh (2018) and the Du Vigneaud Award of the American Peptide Society (2019). She is a member of the National Academy of Science Leopoldina in Germany and was awarded with the Saxonian Order of Merit in 2017.
Acknowledgement
We acknowledge the use of the Protein Data Bank (https://www.rcsb.org/) and the support of Stefanie Babilon for microscopic images.
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Author contributions: All the authors have accepted responsibility for the entire content of this submitted manuscript and approved submission.
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Research funding: The financial contribution of the Deutsche Forschungsgemeinschaft DFG, German Research Foundation, project number 421152132, SFB 1423, subprojects A04/B01 is kindly acknowledged. We thank the Fonds der Chemischen Industrie (FCI) for financial support.
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Conflict of interest statement: The authors declare that there are no competing interests associated with the manuscript.
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