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The Journal of Nuclear Medicine Vol. 40 No. 5 883-888
© 1999 by Society of Nuclear Medicine
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Identification of Receptor Ligands with Phage Display Peptide Libraries

Erkki Koivunen, Wadih Arap, Daniel Rajotte, Johanna Lahdenranta and Renata Pasqualini

Department of Biosciences, Division of Biochemistry, University of Helsinki, Viikinkaari, Finland
The Burnham Institute, La Jolla, California

Correspondence: For correspondence or reprints contact: Renata Pasqualini, PhD, The Burnham Institute, 10901 North Torrey Pines Rd., La Jolla, CA 92037.

ABSTRACT

With the development and maturation of the technology of displaying peptides on bacteriophage, it has become possible to isolate peptide ligands to various targets. In the phage display strategy, up to 109 peptides of different permutations are expressed on the surface of filamentous phage. Thus, peptides capable of binding target molecules in vitro and even target tissues in vivo can be identified. In recent years, a series of libraries that display degenerate peptides of different lengths have been constructed, and specific ligands to cell surface receptors, such as integrins, have been isolated. In the in vivo biopanning, peptides targeting distinct organs or tumors have been rescued after intravenous administration of phage libraries into mice. In one application, the isolated peptide ligands have been used to direct a cytotoxic drug to tumor vasculature in mice. Further applications in radioimaging and radiotherapy are being investigated.

Key Words: phage display • peptide libraries • integrins • targeting • biopanning • receptors • ligands




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