Comparative cell uptake study of FITC-/177Lu-labeled RM26 monomer, dimer and trimer on PC-3: improving binding affinity of gastrin releasing peptide receptor (GRPR) antagonist via bivalency/trivalency

被引：0

作者：

Liangang Zhuo

Xia Yang

Wei Liao

Jing Wang

Hailin Wang

Minli Lv

Guanquan Wang

Hu Song

Yue Feng

Yue Chen

Hongyuan Wei

Yuchuan Yang

Peng Zhao

机构：

[1] China Academy of Engineering Physics (CAEP),Institute of Nuclear Physics and Chemistry (INPC)

[2] The Affiliated Hospital Southwest of Medical University,Department of Nuclear Medicine

[3] Higher Education Institutions,Collaborative Innovation Center of Radiation Medicine of Jiangsu

[4] Key Laboratory of Nuclear Medicine and Molecular Imaging of Sichuan Province,undefined

来源：

Journal of Radioanalytical and Nuclear Chemistry | 2019年 / 319卷

关键词：

RM26 peptide; GRPR antagonist; Lu; Peptide multimerization;

D O I：

暂无

中图分类号：

学科分类号：

摘要：

The gastrin releasing peptide receptors (GRPRs) overexpress in various tumors, which provided the opportunity for GRPR targeted tumor radiological diagnosis and therapy. In recent reports, the GPPR antagonists presented superior specific targeting affinity over the agonists. However, antagonists suffer from many shortcomings regarding their binding affinity and biodistribution properties. In this study, we designed the dimer/trimer antagonists to address the radiotherapy requirements. The results showed both of dimer and trimer RM26 derivatives appeared a progressive improvement. This study provided an efficient strategy to improve the tumor accumulation properties for the GRPR antagonist analogs.

引用

页码：881 / 889

页数：8