Synthesis of oxytocin HYNIC derivatives as potential diagnostic agents for breast cancer
| Autor: | Luis M. De León-Rodríguez, Alma D. Miranda-Olvera, Guillermina Ferro-Flores, Martha Pedraza-López, Consuelo Arteaga de Murphy |
|---|---|
| Rok vydání: | 2007 |
| Předmět: |
Time Factors
Phenylalanine Lysine Biomedical Engineering Pharmaceutical Science Bioengineering Breast Neoplasms Oxytocin Residue (chemistry) Mice Breast cancer medicine Animals Humans Amino Acids Radionuclide Imaging Edetic Acid Pharmacology chemistry.chemical_classification Fluorenes Staining and Labeling Chemistry Organic Chemistry Nicotinic Acids Membrane Proteins Organotechnetium Compounds medicine.disease Oxytocin receptor Amino acid Technetium Compounds Hydrazines Biochemistry Radiopharmaceuticals Somatostatin Biotechnology medicine.drug |
| Zdroj: | Bioconjugate chemistry. 18(5) |
| ISSN: | 1043-1802 |
| Popis: | Two synthetic procedures for HYNIC oxytocin labeling were developed: one based on an orthogonal protection approach and the other with prelabeled (Boc)HYNIC-(Fmoc) amino acids. Both procedures were compared and applied to the preparation of several HYNIC-oxytocin derivatives where ligand position and amino acid (lysine and phenylalanine) were varied. Additionally, an oxytocin derivative labeled with HYNIC in the alpha-amino group of the Cys1 residue was also prepared. 99mTc-ethylendiaminediacetic acid (EDDA) labeling efficiencies were examined for all the derivatives, resulting in two candidates which showed affinity for the oxytocin receptor. Further biochemical experiments demonstrated that 99mTc-EDDA/HYNIC-Cys1-OT-CONH2 could be used as a potential radiopharmaceutical for breast cancer diagnosis. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|