Relaxin family peptides: structure–activity relationship studies

NA Patil; KJ Rosengren; F Separovic; JD Wade; RAD Bathgate; MA Hossain

Journal article

Relaxin family peptides: structure–activity relationship studies

NA Patil, KJ Rosengren, F Separovic, JD Wade, RAD Bathgate, MA Hossain

British Journal of Pharmacology | WILEY | Published : 2017

DOI: 10.1111/bph.13684

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Abstract

The human relaxin peptide family consists of seven cystine-rich peptides, four of which are known to signal through relaxin family peptide receptors, RXFP1–4. As these peptides play a vital role physiologically and in various diseases, they are of considerable importance for drug discovery and development. Detailed structure–activity relationship (SAR) studies towards understanding the role of important residues in each of these peptides have been reported over the years and utilized for the design of antagonists and minimized agonist variants. This review summarizes the current knowledge of the SAR of human relaxin 2 (H2 relaxin), human relaxin 3 (H3 relaxin), human insulin-like peptide 3 (..

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University of Melbourne Researchers

Frances Separovic Author

Ross Bathgate Author

Akhter Hossain Author

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Funding Acknowledgements

This research was partly funded by NHMRC (Australia) project grants (1023321, 1065481 and 1023078) and ARC linkage grant (LP120100654) to M.A.H., R.A.D.B., J.K.R. and J.D.W., a Florey Foundation Fellowship and Melbourne Research Grant Support Scheme (RGSS) awarded to M.A.H., a University of Melbourne Postgraduate Scholarship and Albert Shimmins postgraduate writing-up award to N.A.P., Australian Future Fellowships to K.J.R. (FT130100890), an NHMRC Principal Research Fellowship to J.D.W. (GNT5018148) and NHMRC Senior Research Fellowship to R.A.D.B. (GNT1042650). We acknowledge financial support from Assoc. Prof. Anthony Hughes (Melbourne University) and Dr Johannes Grosse (Takeda Cambridge) through the Linkage grant project. Research at The Florey Institute of Neuroscience and Mental Health is supported by the Victorian Government Operational Infrastructure Support Program.