The importance of tryptophan B28 in H2 relaxin for RXFP2 binding and activation

LJ Chan; JD Wade; F Separovic; RAD Bathgate; MA Hossain

Journal article

The importance of tryptophan B28 in H2 relaxin for RXFP2 binding and activation

LJ Chan, JD Wade, F Separovic, RAD Bathgate, MA Hossain

International Journal of Peptide Research and Therapeutics | SPRINGER | Published : 2013

DOI: 10.1007/s10989-012-9332-x

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Abstract

H2 relaxin (relaxin) is a member of the insulin-relaxin superfamily and exhibits several non-reproductive functions in addition to its well-known properties as a pregnancy hormone. Over the years, the therapeutic potential of relaxin has been examined for a number of conditions. It is currently in phase III clinical trials for the treatment of acute heart failure. The 53 amino acid peptide hormone consists of two polypeptide chains (A and B) which are cross-linked by two inter-chains and one intra-A chain disulfide bridge. Although its cognate receptor is relaxin family peptide receptor (RXFP) 1, relaxin is also able to cross-react with RXFP2, for which the native ligand is INSL3. The "RXXXR..

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University of Melbourne Researchers

Frances Separovic Author

Ross Bathgate Author

Akhter Hossain Author

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Grants

Awarded by National Health and Medical Research Council

Funding Acknowledgements

We thank Tania Ferraro and Sharon Layfield for their assistance with the biochemical assays. This work was supported by an NHMRC Grant (APP #1023078) to JDW, RADB and MAH, and (APP #1023321) to MAH. JDW and RADB are recipients of NHMRC Principal and Senior Research Fellowships, respectively. Studies at the FNI were supported by the Victorian Government's Operational Infrastructure Support Program.