Conjugate Chemistry and Cellular Processing of EGF-Dextran
| Autor: | Jan-Erik Westlin, Per-Uno Malmström, Lars Gedda, Vladimir Tolmachev, Erik Blomquist, Hans Lundqvist, Åsa Liljegren, Anders Sundin, Qinghai Zhao, Anna Sjöström, Jörgen Carlsson |
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| Rok vydání: | 1999 |
| Předmět: |
medicine.medical_treatment
Reductive amination Aldehyde Iodine Radioisotopes chemistry.chemical_compound Epidermal growth factor Tumor Cells Cultured medicine Humans Radiology Nuclear Medicine and imaging Epidermal growth factor receptor chemistry.chemical_classification Epidermal Growth Factor biology Growth factor Dextrans Hematology General Medicine ErbB Receptors Dextran Oncology chemistry Immunology biology.protein Biophysics Astatine Intracellular Conjugate |
| Zdroj: | Acta Oncologica. 38:313-321 |
| ISSN: | 1651-226X 0284-186X |
| DOI: | 10.1080/028418699431384 |
| Popis: | Conjugates with specific binding to the epidermal growth factor receptor, EGFR, of interest for radionuclide based imaging and therapy were prepared using mouse epidermal growth factor, mEGF, and dextran. In one type of conjugate, mEGF was coupled to dextran by reductive amination in which the free amino group on the mEGF N-terminal reacted with the aldehyde group on the reductive end of dextran. The end-end coupled conjugate could be further activated by the cyanopyridinium agent CDAP, thereby introducing tyrosines to the dextran part. In the other type of conjugate, the cyanylating procedure using CDAP was applied, first to activate dextran and then allowing for the amino terminus of mEGF to randomly attach to the dextran. In the latter case, radionuclide-labelled tyrosines or glycines could be added in the same conjugation step. All types of mEGF-dextran conjugates had EGFR-specific binding since the binding could be displaced by an excess of non-radioactive mEGF. The conjugates were to a large extent internalized in the test cells and the associated radioactivity was retained intracellularly for different times depending on both the type of cells and conjugate applied. Different intracellular 'traffic routes' for the radionuclides are discussed as well as applications for both imaging and therapy. |
| Databáze: | OpenAIRE |
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