Design and development of analogues of dimers of insulin-like peptide 3 B-chain as high-affinity antagonists of the RXFP2 receptor.

F Shabanpoor; S Zhang; RA Hughes; MA Hossain; S Layfield; T Ferraro; RAD Bathgate; F Separovic; JD Wade

Journal article

Design and development of analogues of dimers of insulin-like peptide 3 B-chain as high-affinity antagonists of the RXFP2 receptor.

F Shabanpoor, S Zhang, RA Hughes, MA Hossain, S Layfield, T Ferraro, RAD Bathgate, F Separovic, JD Wade

Biopolymers | WILEY-BLACKWELL | Published : 2011

DOI: 10.1002/bip.21484

Abstract

Insulin-like peptide 3 (INSL3) is one of 10 members of the human relaxin-insulin superfamily of peptides. It is a peptide hormone that is expressed by fetal and postnatal testicular Leydig cells and postnatal ovarian thecal cells. It mediates testicular descent during fetal life and suppresses sperm apoptosis in adult males, whereas, in females, it causes oocyte maturation. INSL3 has also been shown to promote thyroid tumor growth and angiogenesis in human. These actions of INSL3 are mediated through its G protein-coupled receptor, RXFP2. INSL3, a two-chained peptide, binds to its receptor primarily via its B-chain, whereas elements of the A-chain are essential for receptor activation. In an..

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University of Melbourne Researchers

Akhter Hossain Author

Ross Bathgate Author

Frances Separovic Author

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Grants

Awarded by National Health and Medical Research Council of Australia

Funding Acknowledgements

[ "Contract grant sponsor: National Health and Medical Research Council of Australia Project", "Contract grant numbers: 350245, 509048", "Fazel Shabanpoor is a recipient of David Hay Postgraduate Write-up award from the University of Melbourne. We thank Linda Chan for the amino acid analyses." ]