Reardan D T, Meares C F, Goodwin D A, McTigue M, David G S, Stone M R, Leung J P, Bartholomew R M, Frincke J M
Nature. 1985;316(6025):265-8. doi: 10.1038/316265a0.
Because monoclonal antibodies can recognize and bind to specific groups of atoms such as tumour antigens, they have promise for use in vivo as carriers of radionuclides, drugs or other appended molecules for diagnosis and treatment of disease. Attachment of metal ions to antibodies by means of bifunctional chelating agents can add the diverse nuclear, physical and chemical properties of the metallic elements to these specific binding proteins (ref. 4 and refs therein). With the ultimate aim of engineering probe-binding properties into the antibodies themselves, we have now prepared monoclonal antibodies against the EDTA chelate of indium. These antibodies show a remarkable preference for indium chelates; changing to another metal such as scandium or gallium can decrease the antibody-binding constant by more than three orders of magnitude. These antibodies also introduce a new degree of control over the biological distributions of chelated radionuclides, markedly altering their uptake in tumours and normal organs.
由于单克隆抗体能够识别并结合特定的原子基团，如肿瘤抗原，因此它们有望在体内用作放射性核素、药物或其他附加分子的载体，用于疾病的诊断和治疗。通过双功能螯合剂将金属离子附着到抗体上，可以将金属元素的各种核、物理和化学性质赋予这些特异性结合蛋白（参考文献4及其中引用的文献）。为了最终将探针结合特性设计到抗体本身中，我们现已制备了针对铟的乙二胺四乙酸（EDTA）螯合物的单克隆抗体。这些抗体对铟螯合物表现出显著的偏好；换成另一种金属，如钪或镓，会使抗体结合常数降低三个以上数量级。这些抗体还对螯合放射性核素的生物分布引入了新的控制程度，显著改变了它们在肿瘤和正常器官中的摄取。
