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Identification and characterization of a novel peptide ligand of epidermal growth factor receptor for targeted delivery of therapeutics

Zonghai Li^*,, Ruijiao Zhao^*, Xianghua Wu^*,, Ye Sun, Ming Yao^*, Jinjun Li^*, Yuhong Xu^*,,1 and Jianren Gu^*,,1

^* National Laboratory for Oncogenes and Related Genes, Shanghai Cancer Institute, Medical College of and
School of Pharmacy, Shanghai Jiao Tong University, Shanghai, China; and
Medical college of Fudan University, Shanghai, China

¹Correspondence: National Laboratory for Oncogenes and Related Genes, Shanghai Cancer Institute, No.25/2200, Xietu Road, Shanghai 200032, China. E-mail: yhxu@sjtu.edu.cn or nlorg{at}sh163.net

Epidermal growth factor receptor (ErbB1, EGFR) is overexpressed in a variety of human cancer cells. It has been considered as a rational target for drug delivery. To identify novel ligands with specific binding capabilities to EGFR, we screened a phage display peptide library and found an enriched phage clone encoding the amino acid sequence YHWYGYTPQNVI (designated as GE11). Competitive binding assay and Scatchard analysis revealed that GE11 peptide bound specifically and efficiently to EGFR with a dissociation constant of 22 nM, but with much lower mitogenic activity than with EGF. We showed that the peptides were internalized preferentially into EGFR highly expressing cells, and they accumulated in EGFR overexpressing tumor xenografts after i.v. delivery in vivo. In gene delivery studies, GE11-conjugated polyethylenimine (PEI) vectors were less mitogenic, but still quite efficient at transfecting genes into EGFR highly expressing cells and tumor xenografts. Taken together, GE11 is a potentially safe and efficient targeting moiety for selective drug delivery systems mediated through EGFR.—Li, Z., Zhao, R., Wu, X., Sun, Y., Yao, M., Li, J., Xu, Y., Gu, J. Identification and characterization of a novel peptide ligand of epidermal growth factor receptor for targeted delivery of therapeutics.

Key Words: EGFR • peptide synthesis • peptide ligand

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