Journal article

The chemically synthesized human relaxin-2 analog, B-R13/17K H2, is an RXFP1 antagonist

MA Hossain, CS Samuel, C Binder, TD Hewitson, GW Tregear, JD Wade, RAD Bathgate

Amino Acids | SPRINGER | Published : 2010

Abstract

Relaxin is a pleiotropic hormone which exerts its biological functions through its G-protein coupled receptor, RXFP1. While relaxin is well known for its reproductive and antifibrotic roles, recent studies suggest that it is produced by cancer cells and acts on RXFP1 to induce growth and metastasis. Furthermore, more recently Silvertown et al. demonstrated that lentiviral production of a human gene-2 (H2) relaxin analog reduced the growth of prostate xenograft tumors. The authors proposed that the lentivirally produced peptide was an RXFP1 antagonist; however, the processed form of the peptide produced was not demonstrated. In this study, we have chemically synthesized the H2 relaxin analog,..

View full abstract

Grants

Awarded by National Health and Medical Research Council


Funding Acknowledgements

This study was funded by a grant to JDW, GWT, and RADB from the National Health and Medical Research Council (NHMRC) of Australia (ID no. 508995). RADB, JDW, and GWT are recipients of Research Fellowship from the NHMRC, while CSS is the recipient of a National Heart Foundation of Australia/NHMRC RD Wright Fellowship. We would like to thank Sharon Layfield and Tania Ferraro for performing the binding and the cAMP assays, Matthias Schulz for technical assistance with the MCF-7 invasion assays, and Ishanee Mookerjee for assistance with the renal myofibroblast differentiation assays.