title: Hybrid bombesin analogues: combining an agonist and an antagonist in defined distances for optimized tumor targeting.
abstract: Radiolabeled hybrid ligands with defined distances between an agonist and an antagonist for the gastrin-releasing peptide receptor were found to have excellent tumor-targeting properties. Oligoprolines served as rigid scaffolds that allowed for tailoring distances of 10, 20, and 30 Å between the recognition elements. In vitro and in vivo studies revealed that the hybrid ligand with a distance of 20 Å between the recognition elements exhibits the highest yet observed tumor cell uptake and retention time in prostate cancer cells.
authors.affiliation: Laboratory of Organic Chemistry, ETH Zürich , Zürich, Switzerland.
authors.forename: Carsten
authors.initials: C
authors.lastname: Kroll
authors.forename: Rosalba
authors.initials: R
authors.lastname: Mansi
authors.forename: Friederike
authors.initials: F
authors.lastname: Braun
authors.forename: Stefanie
authors.initials: S
authors.lastname: Dobitz
authors.forename: Helmut R
authors.initials: HR
authors.lastname: Maecke
authors.forename: Helma
authors.initials: H
authors.lastname: Wennemers
mesh_terms: D000818:Animals; D001839:Bombesin / Q000031:analogs & derivatives* / Q000493:pharmacokinetics*; D045744:Cell Line, Tumor; D016503:Drug Delivery Systems; D006801:Humans; D008297:Male; D051379:Mice; D008819:Mice, Nude; D011392:Proline / Q000031:analogs & derivatives / Q000493:pharmacokinetics; D011471:Prostatic Neoplasms / Q000188:drug therapy*; D018004:Receptors, Bombesin / Q000819:agonists* / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D018004:Receptors, Bombesin; D011392:Proline; D001839:Bombesin