Investigation of interactions at the extracellular loops of the relaxin family peptide receptor 1 (RXFP1)

NA Diepenhorst; EJ Petrie; CZ Chen; A Wang; MA Hossain; RAD Bathgate; PR Gooley

Journal article

Investigation of interactions at the extracellular loops of the relaxin family peptide receptor 1 (RXFP1)

NA Diepenhorst, EJ Petrie, CZ Chen, A Wang, MA Hossain, RAD Bathgate, PR Gooley

Journal of Biological Chemistry | AMER SOC BIOCHEMISTRY MOLECULAR BIOLOGY INC | Published : 2014

DOI: 10.1074/jbc.M114.600882

Abstract

Relaxin, an emerging pharmaceutical treatment for acute heart failure, activates the relaxin family peptide receptor (RXFP1), which is a classAG-protein-coupled receptor. In addition to the classic transmembrane (TM) domain, RXFP1 possesses a large extracellular domain consisting of 10 leucine-rich repeats and an N-terminal low density lipoprotein class A (LDLa) module. Relaxin-mediated activation of RXFP1 requires multiple coordinated interactions between the ligand and various receptor domains including a high affinity interaction involving the leucine-rich repeats and a predicted lower affinity interaction involving the extracellular loops (ELs). The LDLa is essential for signal activatio..

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University of Melbourne Researchers

Akhter Hossain Author

Ross Bathgate Author

Paul Gooley Author

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Grants

Awarded by National Health and Medical Research Council of Australia

Funding Acknowledgements

[ "This work was supported by National Health and Medical Research Council of Australia Project Grants 628427 and 1043750 (to R. A. D. B. and P. R. G.) by the Victorian Government Operational Infrastructure Support Program, and through instrument funding from the State of Victoria, Australian Research Council, and the Rowden White Foundation.", "Recipient of a Melbourne Research Fellowship (Career Interruptions).", "Recipient of a National Health and Medical Research Council Research Fellowship. To whom correspondence may be addressed: Florey Inst. of Neuroscience and Mental Health, University of Melbourne, Parkville, Victoria 3010, Australia. Tel.: 61-3-9035-6735; E-mail: bathgate@florey.edu.au." ]