Synthesis of oxytocin HYNIC derivatives as potential diagnostic agents for breast cancer
Synthesis of oxytocin HYNIC derivatives as potential diagnostic agents for breast cancer
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DOI：
10.1021/bc070047a
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发表时间：
2007-09-01
影响因子：
4.7
通讯作者：
De Leon-Rodriguez, Luis M.
中科院分区：
文献类型：
--
作者：
Miranda-Olvera, Alma D.;Ferro-Flores, Guillermina;De Leon-Rodriguez, Luis M.
HYNIC催产素标记的两个合成程序开发：一个基于正交保护的方法和其他预标记（Boc）HYNIC-（Fmoc）氨基酸。这两种程序进行了比较，并适用于制备几个HYNIC-催产素衍生物，其中配体的位置和氨基酸（赖氨酸和苯丙氨酸）是不同的。此外，还制备了在Cys（1）残基的α-氨基中用HYNIC标记的催产素衍生物。Tc-99 m-乙二胺二乙酸（EDDA）标记效率进行了检查，所有的衍生物，产生两个候选人，显示出对催产素受体的亲和力。进一步的生物化学实验表明，Tc-99 m-EDDA/HYNIC-Cys（1）-OT-CONH 2可作为一种潜在的乳腺癌诊断放射性药物。
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 Cys(1) residue was also prepared. Tc-99m-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 Tc-99m-EDDA/HYNIC-Cys(1)-OT-CONH2 could be used as a potential radiopharmaceutical for breast cancer diagnosis.