Signalling profiles of H3 relaxin, H2 relaxin and R3(BΔ23-27)R/I5 acting at the relaxin family peptide receptor 3 (RXFP3)

M Kocan; M Sarwar; MA Hossain; JD Wade; RJ Summers

Journal article

Signalling profiles of H3 relaxin, H2 relaxin and R3(BΔ23-27)R/I5 acting at the relaxin family peptide receptor 3 (RXFP3)

M Kocan, M Sarwar, MA Hossain, JD Wade, RJ Summers

British Journal of Pharmacology | WILEY | Published : 2014

DOI: 10.1111/bph.12623

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Abstract

Background and Purpose Relaxin family peptide receptor 3 (RXFP3) is expressed in brain areas important for processing sensory information and feeding, suggesting that it may be a target for anti-anxiety and anti-obesity drugs. We examined the effects of H3 relaxin, the biased agonist H2 relaxin and the antagonist, R3(BΔ23-27)R/I5, on RXFP3 signalling to establish their suitability as tools to assess the physiological roles of RXFP3. Experimental Approach The signalling profile of the RXFP3 ligands was determined using reporter gene assays, multiplexed signalling assays and direct examination of receptor-G protein and receptor-β-arrestin interactions using BRET. Key Results H2 relaxin activat..

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Akhter Hossain Author

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Funding Acknowledgements

We thank Dr Nathan Hall for images of peptide structures and Dr Caroline Hick for expert technical advice. We are grateful to A/Prof Ross Bathgate (Florey Institute of Neuroscience and Mental Health), A/Prof Kevin Pfleger (Western Australian Institute for Medical Research and Centre for Medical Research, University of Western Australia) and Dr Bronwyn Evans for useful scientific discussions and advices. Studies carried out at the Florey Institute of Neuroscience and Mental Health were supported by the Victorian Government's Operational Infrastructure Support Program. We are grateful to Andreas Loening and Sanjiv Gambhir (Stanford University, Stanford, CA), Atsushi Miyawaki (RIKEN Brain Science Institute, Wako City, Japan) and Michel Bouvier (Department of Biochemistry, Universite de Montreal, Montreal, Quebec, Canada) for providing cDNA constructs. This research was supported by the National Health and Medical Research Council (NH&MRC Australia Project Grants 436713, 454375 and Program Grant 519461).