A practical guide to the construction of radiometallated bioconjugates for positron emission tomography.
A practical guide to the construction of radiometallated bioconjugates for positron emission tomography.
复制标题
DOI：
10.1039/c0dt01595d
复制
发表时间：
2011-06-21
期刊：
影响因子：
--
通讯作者：
Lewis JS
中科院分区：
文献类型：
--
作者：
Zeglis BM;Lewis JS
正电子发射断层扫描 (PET) 已成为诊断和治疗疾病（尤其是癌症）的重要成像方式。现已开发出多种小分子 PET 放射性示踪剂，采用短半衰期放射性核素 11C、13N、15O 和 18F。然而，基于生物分子靶向载体的 PET 放射性药物已成为实验室和临床研究急剧增加的主题。通常基于抗体、寡肽或寡核苷酸，这些示踪剂比其小分子对应物具有更长的生物半衰期，因此需要用具有更长、互补放射性半衰期的放射性核素进行标记，例如金属同位素 64Cu、68Ga、86Y 和 89Zr。每种生物共轭放射性药物都有四个组成部分：生物分子载体、放射性金属、螯合剂以及螯合剂和生物分子之间的共价连接。除了放射性金属之外，这些片段中的每一个都存在多种选择，并且已经利用大量不同的螯合、缀合和放射性金属化策略来创建从 68Ga 标记的五肽到 89Zr 标记的单克隆抗体的试剂。在此，作者提出了构建基于放射性金属的 PET 生物共轭物的实用指南，其中文献中各种生物分子示踪剂的设计选择和合成细节都收集在一个参考文献中。在汇总这些信息时，作者希望既能阐明合成这些药物所采用的多种方法，又能为该领域经验丰富和新手的分子成像研究人员提供有用的参考。
Positron emission tomography (PET) has become a vital imaging modality in the diagnosis and treatment of disease, most notably cancer. A wide array of small molecule PET radiotracers have been developed that employ the short half-life radionuclides 11C, 13N, 15O, and 18F. However, PET radiopharmaceuticals based on biomolecular targeting vectors have been the subject of dramatically increased research in both the laboratory and the clinic. Typically based on antibodies, oligopeptides, or oligonucleotides, these tracers have longer biological half-lives than their small molecule counterparts and thus require labeling with radionuclides with longer, complementary radioactive half-lives, such as the metallic isotopes 64Cu, 68Ga, 86Y, and 89Zr. Each bioconjugate radiopharmaceutical has four component parts: biomolecular vector, radiometal, chelator, and covalent link between chelator and biomolecule. With the exception of the radiometal, a tremendous variety of choices exists for each of these pieces, and a plethora of different chelation, conjugation, and radiometallation strategies have been utilized to create agents ranging from 68Ga-labeled pentapeptides to 89Zr-labeled monoclonal antibodies. Herein, the authors present a practical guide to the construction of radiometal-based PET bioconjugates, in which the design choices and synthetic details of a wide range of biomolecular tracers from the literature are collected in a single reference. In assembling this information, the authors hope both to illuminate the diverse methods employed in the synthesis of these agents and also to create a useful reference for molecular imaging researchers both experienced and new to the field.
登录
查看更多内容
影响因子：
2.8
作者：
Amin, S;Marks, C;Morrow, JR
通讯作者：
Morrow, JR
影响因子：
3.1
作者：
Asti, Mattia;De Pietri, Giovanni;Salvo, Diana
通讯作者：
Salvo, Diana
影响因子：
4.6
作者：
BERNHARDT, PV;BRAMLEY, R;WHITE, AH
通讯作者：
WHITE, AH
影响因子：
4.6
作者：
BEVILACQUA, A;GELB, RI;ZOMPA, LJ
通讯作者：
ZOMPA, LJ
影响因子：
1.6
作者：
Abbas, K.;Kozempel, J.;Gibson, N.
通讯作者：
Gibson, N.