title: Peptide-receptor ligands and multivalent approach.
abstract: The overexpression of peptide receptors in human tumours makes peptide-ligands attractive agents for the development of specific diagnostic imaging and/or therapy of cancers. Solid-phase peptide synthesis, modern phage display technology and combinatorial peptide chemistry have profoundly affected the pool of available targeting peptides for efficient and specific delivery of imaging or therapeutic label molecules. Additionally, the availability of a wide range of bifunctional chelating agents for the radiolabelling of bioactive peptides with radionuclides has produced a wide variety of useful radiopharmaceutical molecules. This review article examines the principal receptors-binding peptides and their overexpression on tumour cells. We discuss the advantage and the challenges in developing multivalent peptide-based ligands summarising their design strategies and applications.
authors.affiliation: Institute of Biomolecular Chemistry of CNR, Padova Unit, via Marzolo 1, 35131 Padova, Italy. paolo.ruzza@unipd.it
authors.forename: Paolo
authors.initials: P
authors.lastname: Ruzza
authors.forename: Anna
authors.initials: A
authors.lastname: Marchiani
authors.forename: Nicola
authors.initials: N
authors.lastname: Antolini
authors.forename: Andrea
authors.initials: A
authors.lastname: Calderan
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D015972:Gene Expression Regulation, Neoplastic; D006801:Humans; D008024:Ligands; D008969:Molecular Sequence Data; D009369:Neoplasms / Q000175:diagnosis* / Q000235:genetics* / Q000378:metabolism; D018000:Receptors, Peptide / Q000032:analysis* / Q000737:chemistry / Q000235:genetics* / Q000378:metabolism
chemical_list: D008024:Ligands; D018000:Receptors, Peptide