caa a22 4500 477126324 CHVBK 20180405111650.0 cr unu---uuuuu 170330e19970701xx s 000 0 eng 10.1023/A:1012195615944 doi (NATIONALLICENCE)springer-10.1023/A:1012195615944 Tyramine-Containing Poly(4-Nitrophenylacrylate) as lodinatable Ligand Carrier in Biodistribution Analysis [Elektronische Daten] [Shuji Kojima, Sabine André, Elena Korchagina, Nicolai Bovin, Hans-Joachim Gabius] Purpose. Targeted label or drug delivery requires access to convenient carrier systems and methods for efficient ligand conjugation. The main purpose of this study is to design an iodinatable synthetic polymer, whose application in vivo in tumor-bearing mice is tested with several related carbohydrate ligands, namely ABH and Lewis blood group epitopes. Methods. Tyramine and aminopropyl derivatives of the synthetic oligo-saccharides were attached to poly(4-nitrophenylacrylate). Following iodination, the biodistribution of the sugar-free and the substituted polymers was determined in tumor-bearing mice. Flow cytofluorimetric analysis assessed tumor cell binding of further ligand types to human tumor cells in vitro. Results. Quantitative ligand incorporation was achieved under mild conditions. Whereas the ligand-free poly[N-(2-hydroxyethyl)acrylamide] (MW 30 kDa) showed preferential accumulation in kidney, neoglycopolymers were found in substantial amounts in liver, kidney or spleen. The nature of the carbohydrate structure quantitatively influenced the distribution pattern. Tumor cell binding of blood group determinants and three further ligand types revealed non-uniform intensity in labeling and percentage of positive cells even in comparison between lines with identical histogenetic origin. Conclusions. Carbohydrate-exposing poly[N-(2-hydroxyethyl)acrylamide] polymers with tyramine as an iodine acceptor distribute in mice with a profile which is quantitatively influenced by small structural variations of the ligand part. Further refinement of the ligand structure may increase the level of selectivity for organ and tumor accumulation. Plenum Publishing Corporation, 1997 radiopharmaceutical nationallicence imaging nationallicence targeting nationallicence neoglyco-conjugate nationallicence lectin nationallicence tumor cell nationallicence Kojima Shuji Department of Biomedical Science-1, Research Institute for Biosciences, Science University of Tokyo, 2669 Yamazaki, Noda-Shi, 278, Chiba, Japan aut André Sabine Institute of Physiological Chemistry, Faculty of Veterinary Medicine, Ludwig-Maximilians-University, Veterinärstr. 13, D-80539, München, Germany aut Korchagina Elena Shemyakin Institute of Bioorganic Chemistry, Russian Academy of Sciences, ul, Miklukho-Maklaya 16/10, Moscow, Russian Federation aut Bovin Nicolai Shemyakin Institute of Bioorganic Chemistry, Russian Academy of Sciences, ul, Miklukho-Maklaya 16/10, Moscow, Russian Federation aut Gabius Hans-Joachim Institute of Physiological Chemistry, Faculty of Veterinary Medicine, Ludwig-Maximilians-University, Veterinärstr. 13, D-80539, München, Germany aut Pharmaceutical Research Kluwer Academic Publishers-Plenum Publishers 14/7(1997-07-01), 879-886 0724-8741 14:7<879 1997 14 11095 https://doi.org/10.1023/A:1012195615944 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1023/A:1012195615944 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Kojima Shuji Department of Biomedical Science-1, Research Institute for Biosciences, Science University of Tokyo, 2669 Yamazaki, Noda-Shi, 278, Chiba, Japan aut NATIONALLICENCE 700 1- André Sabine Institute of Physiological Chemistry, Faculty of Veterinary Medicine, Ludwig-Maximilians-University, Veterinärstr. 13, D-80539, München, Germany aut NATIONALLICENCE 700 1- Korchagina Elena Shemyakin Institute of Bioorganic Chemistry, Russian Academy of Sciences, ul, Miklukho-Maklaya 16/10, Moscow, Russian Federation aut NATIONALLICENCE 700 1- Bovin Nicolai Shemyakin Institute of Bioorganic Chemistry, Russian Academy of Sciences, ul, Miklukho-Maklaya 16/10, Moscow, Russian Federation aut NATIONALLICENCE 700 1- Gabius Hans-Joachim Institute of Physiological Chemistry, Faculty of Veterinary Medicine, Ludwig-Maximilians-University, Veterinärstr. 13, D-80539, München, Germany aut NATIONALLICENCE 773 0- Pharmaceutical Research Kluwer Academic Publishers-Plenum Publishers 14/7(1997-07-01), 879-886 0724-8741 14:7<879 1997 14 11095 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer