title: MSH radiopeptides for targeting melanoma metastases.
abstract: Radiolabeled peptides have become important tools for preclinical cancer research and in nuclear oncology they serve as diagnostic and more recently also as therapeutic agents. Whereas the development of receptor-mediated targeting for therapy has been confined to some radiolabeled antibodies and somatostatin/SRIF analogs, recent research into radiolabeled α-Melanocyte-stimulating hormone (α-MSH) and its receptor MC1R (over-)expressed by melanoma tumor cells has demonstrated that small metastatic melanoma lesions in experimental animals are specifically targeted by MSH radiopeptides. Thus MSH radiopharmaceuticals will eventually open a new avenue for the treatment of melanoma metastases in man, provided that the targeting efficiency can be further enhanced and nonspecific incorporation into nontarget organs, e.g., the kidneys, minimized. Some novel MSH lead compounds containing a glyco moiety, added negatively charged groups or a cyclic structure show very promising in vivo targeting characteristics.
authors.affiliation: Laboratory of Endocrinology, Department of Biomedicine, University Hospital Basel and University Children's Hospital, University of Basel, Klingelbergstrasse 23, CH-4031, Basel, Switzerland. alex-n.eberle@unibas.ch
authors.forename: Alex N
authors.initials: AN
authors.lastname: Eberle
authors.forename: Jean-Philippe
authors.initials: JP
authors.lastname: Bapst
authors.forename: Martine
authors.initials: M
authors.lastname: Calame
authors.forename: Heidi
authors.initials: H
authors.lastname: Tanner
authors.forename: Sylvie
authors.initials: S
authors.lastname: Froidevaux
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D006801:Humans; D009074:Melanocyte-Stimulating Hormones / Q000737:chemistry / Q000378:metabolism*; D008545:Melanoma / Q000175:diagnosis / Q000378:metabolism / Q000473:pathology* / Q000532:radiotherapy*; D058990:Molecular Targeted Therapy / Q000379:methods*; D009362:Neoplasm Metastasis; D010446:Peptide Fragments / Q000737:chemistry / Q000378:metabolism* / Q000627:therapeutic use*; D019275:Radiopharmaceuticals / Q000737:chemistry / Q000378:metabolism / Q000627:therapeutic use*
chemical_list: D010446:Peptide Fragments; D019275:Radiopharmaceuticals; D009074:Melanocyte-Stimulating Hormones