Abstract
Relaxin-3 and its endogenous receptor RXFP3 are involved in fundamental neurological signalling pathways, such as learning and memory, stress, feeding and addictive behaviour. Consequently, this signalling system has emerged as an attractive drug target. Development of leads targeting RXFP3 relies on assays for screening and ligand optimization. Here, we present the synthesis and in vitro characterization of a fluorescent europium-labelled antagonist of RXFP3. This ligand represents a cheap and safe but powerful tool for future mechanistic and cell-based receptor–ligand interaction studies of the RXFP3 receptor.
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Acknowledgments
K. J. R. is an ARC Future Fellow and R. A. D. B an NHMRC (Australia) Senior Research Fellow, respectively. This work was supported by NHMRC project grants APP1066369 and APP1065481 to K. J. R and R. A. D. B. Research at The Florey Institute of Neuroscience and Mental Health was supported by the Victorian Government Operational Infrastructure Support Program.
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The authors declare that they have no conflict of interests.
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Haugaard-Kedström, L.M., Wong, L.L.L., Bathgate, R.A.D. et al. Synthesis and pharmacological characterization of a europium-labelled single-chain antagonist for binding studies of the relaxin-3 receptor RXFP3. Amino Acids 47, 1267–1271 (2015). https://doi.org/10.1007/s00726-015-1961-x
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DOI: https://doi.org/10.1007/s00726-015-1961-x