RXFP1 couples to the Gαi3-Gβγ-PI3K-PKCζ pathway via the final 10 amino acids of the receptor C-terminal tail

ML Halls; M Papaioannou; JD Wade; BA Evans; RAD Bathgate; RJ Summers

Conference Proceedings

RXFP1 couples to the Gαi3-Gβγ-PI3K-PKCζ pathway via the final 10 amino acids of the receptor C-terminal tail

ML Halls, M Papaioannou, JD Wade, BA Evans, RAD Bathgate, RJ Summers

Annals of the New York Academy of Sciences | WILEY-BLACKWELL | Published : 2009

DOI: 10.1111/j.1749-6632.2008.03813.x

Abstract

The relaxin family peptide receptors RXFP1 and RXFP2 are highly similar receptors that share approximately 80% amino acid sequence homology. Constitutively active receptors couple to increased cAMP accumulation, which is important for relaxin-mediated decidualization and myometrial inhibition. Despite the high homology, the receptors couple to different G-proteins to affect cAMP accumulation. This study aimed to determine the region of RXFP1 that directs coupling to the delayed Gαi3 pathway by using receptor mutagenesis. Receptor chimeras suggested that activation of this pathway by RXFP1 was dependent upon the membrane-anchored domain of the receptor. Further receptor mutagenesis showed tha..

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University of Melbourne Researchers

Ross Bathgate Author

Related Projects (1)

Novel G-protein coupled receptors LGR7 and LGR8; the receptors for relaxin and insulin-like peptide 3 (INSL3)

Relaxin is a hormone which has long been known to have essential roles in pregnancy and birth. However it has also been demonstrated to have..

Grants

Awarded by National Health and Medical Research Council (NHMRC)

Awarded by ARC

Awarded by Australian Research Council

Funding Acknowledgements

This work was supported in part by National Health and Medical Research Council (NH&MRC) Block Grant Reg Key 983001 to the Howard Florey Institute, NH&MRC project grants 300012 (RADB and RJS), 436713 (RJS and RADB), and ARC Linkage Grant LP0560620 (RJS and RADB). MLH is a recipient of an NH&MRC Overseas Biomedical Fellowship and a Relaxin 2008 Young Investigator Award.