期刊
JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
卷 317, 期 3, 页码 1243-1252出版社
SPRINGER
DOI: 10.1007/s10967-018-6013-z
关键词
Doxorubicin; Radioidination; Tumor imaging; Molecular dynamics; Molecular docking
资金
- Westgrid
- Compute/Calcul Canada
Non-invasive molecular imaging techniques are accruing more interest in the last decades. Several radiolabelling elements have been FDA-approved and are currently used to characterize tumors. In this study, the DNA intercalating agent doxorubicin was radiolabelled with I-125. Several parameters for the radiolabelling reaction were investigated and optimized. A maximum yield of 94 +/- 0.3% was reached after reacting 20 mu g of doxorubicin with 200 mu g Chloramine-T at pH 5 for 30 min. The in vivo stability of I-125-doxorubicin is validated by the low propensity for thyroid uptake in mice. The preclinical T/NT ratio was approximately 6.4 at 30 min. Docking and molecular dynamics confirmed that the radiolabelling of doxorubicin did not affect (or slightly improved its binding to DNA). Overall, I-125-doxorubicin was demonstrated to be a promising non-invasive probe for solid tumor imaging. [GRAPHICS] .
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据