PMID: 8608180Nov 1, 1995Paper

A new radioligand for the epidermal growth factor receptor: 111In labeled human epidermal growth factor derivatized with a bifunctional metal-chelating peptide

Bioconjugate Chemistry
S RémyJ Gariépy

Abstract

More specific radiopharmaceuticals are currently being evaluated for the in vivo detection and therapy of breast cancer. The human epidermal growth factor (hEGF) represents a good radiopharmaceutical candidate in view of the reported overexpression of its receptor by breast cancer cells. To enhance the imaging potential of this peptide ligand, a synthetic strategy was developed to rapidly create small peptides containing a large number of metal-chelating groups that can be readily coupled to hEGF. A prototypic 15-amino acid branched peptide containing four EDTA-like chelator groups was assembled by solid phase peptide synthesis. The metal chelating peptide, abbreviated MCP-4-EDTA-SH, was selectively incorporated into hEGF(1-51) at its unique N-terminus amino group. The coupling of a single MCP-4-EDTA-SH into hEGF(1-51) was confirmed by SDS polyacrylamide gel electrophoresis, western blotting, and amino acid analysis. The protein conjugate was successfully labeled with 111In. Its specific binding to EGF receptors present on MDA-MB-468 breast cancer cells confirmed that such a construct retains the properties of the natural ligand.

References

Jan 1, 1990·Progress in Growth Factor Research·W J Gullick
Jul 26, 1989·Journal of Immunological Methods·P R Young
Jul 1, 1984·The Journal of Experimental Medicine·J B RothbardG K Schoolnik
Jan 1, 1994·Breast Cancer Research and Treatment·C F LeMaistreC K Osborne
Jan 1, 1994·Breast Cancer Research and Treatment·J Baselga, J Mendelsohn
May 1, 1959·Archives of Biochemistry and Biophysics·G L ELLMAN

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Citations

Nov 27, 1998·Journal of Immunological Methods·M K BhalgatR P Haugland
Nov 16, 2002·Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine·Ronald E Weiner, Mathew L Thakur
Sep 25, 2003·Cancer Biotherapy & Radiopharmaceuticals·Asa Liljegren SundbergVladimir Tolmachev
Nov 17, 2001·Seminars in Nuclear Medicine·R E Weiner, M L Thakur
Jan 8, 2014·Journal of Labelled Compounds & Radiopharmaceuticals·Bart Cornelissen

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