Synthesis of oxytocin HYNIC derivatives as potential diagnostic agents for breast cancer |
| |
Authors: | Miranda-Olvera Alma D Ferro-Flores Guillermina Pedraza-López Martha de Murphy Consuelo Arteaga De León-Rodríguez Luis M |
| |
Institution: | Instituto de Investigaciones Científicas, Universidad de Guanajuato, Guanajuato, Gto. Mexico. |
| |
Abstract: | 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. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|