Synthesis and evaluation of a bifunctional chelate for development of Bi(III)-labeled radioimmunoconjugates

被引：20

作者：

Dadwal, Mamta ^{[1
]}

Kang, Chi Soo ^{[1
]}

Song, Hyun A. ^{[1
]}

Sun, Xiang ^{[1
]}

Dai, Anzhi ^{[1
]}

Baidoo, Kwamena E. ^{[2
]}

Brechbiel, Martin W. ^{[2
]}

Chong, Hyun-Soon ^{[1
]}

机构：

[1] IIT, Biol Chem & Phys Sci Dept, Div Chem, Chicago, IL 60616 USA

[2] NCI, Radioimmune & Inorgan Chem Sect, Radiat Oncol Branch, Ctr Canc Res,NIH, Bethesda, MD 20892 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 24期

基金：

美国国家卫生研究院;

关键词：

Radioimmunotherapy; Bifunctional ligand; (212)Bi; (213)Bi; Trastuzumab; MYELOID-LEUKEMIA; RADIOIMMUNOTHERAPY; TRASTUZUMAB; ANTIBODIES; ANTI-CD33; THERAPY; BI-213;

D O I：

10.1016/j.bmcl.2011.06.107

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new bifunctional ligand C-DEPA was designed and synthesized as a component for antibody-targeted radiation therapy (radioimmunotherapy, RIT) of cancer. C-DEPA was conjugated to a tumor targeting antibody, trastuzumab, and the corresponding C-DEPA-trastuzumab conjugate was evaluated for radiolabeling kinetics with (205/6)Bi. C-DEPA-trastuzumab conjugate rapidly bound (205/6)Bi, and (205/6)Bi-C-DEPA-trastuzumab conjugate was stable in human serum for 72 h. The in vitro radiolabeling kinetics and serum stability data suggest that C-DEPA is a potential chelate for preclinical RIT applications using (212)Bi and (213)Bi. (C) 2011 Published by Elsevier Ltd.

引用

页码：7513 / 7515

页数：3

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