De novo design and synthesis of cyclic and linear peptides to mimic the binding cassette of human relaxin

MA Hossain; RAD Bathgate; G Tregear; JD Wade

Journal article

De novo design and synthesis of cyclic and linear peptides to mimic the binding cassette of human relaxin

MA Hossain, RAD Bathgate, G Tregear, JD Wade

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

DOI: 10.1111/j.1749-6632.2009.03840.x

Abstract

A synthetic cyclic regioselectively addressable functionalized template was used to prepare six analogs that presented the side chains of the key receptor-binding residues of each of H2 and H3 relaxins and insulin-like peptide 3. None showed any binding affinity for RXFP1, RXFP2, or RXFP3, indicating that the key residues were either incorrectly oriented or that additional residues are required for receptor binding. © 2009 New York Academy of Sciences.

University of Melbourne Researchers

Akhter Hossain Author

Ross Bathgate Author

Related Projects (1)

The structural basis of the interaction of human relaxins with their receptors

Human Gene 2 (H2) relaxin is a peptide hormone structurally related to insulin and has numerous biological actions related to its roles duri..

Grants

Awarded by NHMRC of Australia

Funding Acknowledgements

The work described herein was supported by a project grant to, JDW and RADB (350284) from the NHMRC of Australia. We thank Mary Macris for amino acid analysis and Taina Ferraro and Sharon Layfield for their assistance with the binding assays.