Site-specific conjugation of a lanthanide chelator and its effects on the chemical synthesis and receptor binding affinity of human relaxin-2 hormone

F Shabanpoor; RAD Bathgate; A Belgi; LJ Chan; VB Nair; JD Wade; MA Hossain

Journal article

Site-specific conjugation of a lanthanide chelator and its effects on the chemical synthesis and receptor binding affinity of human relaxin-2 hormone

F Shabanpoor, RAD Bathgate, A Belgi, LJ Chan, VB Nair, JD Wade, MA Hossain

Biochemical and Biophysical Research Communications | ACADEMIC PRESS INC ELSEVIER SCIENCE | Published : 2012

DOI: 10.1016/j.bbrc.2012.02.141

Abstract

Diethylenetriamine pentaacetic acid (DTPA) is a popular chelator agent for enabling the labeling of peptides for their use in structure-activity relationship study and biodistribution analysis. Solid phase peptide synthesis was employed to couple this commercially available chelator at the N-terminus of either the A-chain or B-chain of H2 relaxin. The coupling of the DTPA chelator at the N-terminus of the B-chain and subsequent loading of a lanthanide (europium) ion into the chelator led to a labeled peptide (Eu-DTPA-(B)-H2) in low yield and having very poor water solubility. On the other hand, coupling of the DTPA and loading of Eu at the N-terminus of the A-chain led to a water-soluble pep..

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University of Melbourne Researchers

Ross Bathgate Author

Akhter Hossain Author

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Grants

Awarded by National Health and Medical Research Council

Funding Acknowledgements

This research was funded by NHMRC (Australia) project grants 350284 and 508995 to JDW and RADB. We are grateful to Tania Ferraro & Sharon Layfield for assistance with biochemical assays and to Feng Lin for amino acid analysis. During these studies, MAH was the recipient of a Reid Trust Fellowship, and is currently a Florey Trust Foundation Fellow. RADB is an NHMRC Senior Research Fellow. JDW is an NHMRC Principal Research Fellow. Studies at the FNI were supported by the Victorian Government's Operational Infrastructure Support Program.