Haseman M K, Goodwin D A, Meares C F, Kaminski M S, Wensel T G, McCall M J, Levy R
Eur J Nucl Med. 1986;12(9):455-60. doi: 10.1007/BF00254750.
The relative biological properties of 111In-labeled monoclonal antibodies (MoAb) coupled with a conventional bifunctional chelate (BC) and a new, enzyme metabolizable, bifunctional chelate (BCM) were investigated. A rat IgG2a MoAb against idiotype from a mouse B-cell lymphoma was utilized. Mice bearing B-cell lymphomas in the subcutaneous tissues of the flank were given IV-injections of labeled MoAb and imaged or killed for organ counting at 24 h or 48 h. Rat anti-dinitrophenyl IgG2a MoAb and non-specific polyclonal mouse IgG were used as controls. Compared to BC, the use of BCM resulted in a substantial decrease in blood background activity, a shorter biological half-life and an increase in tumor to blood ratio at the expense of a moderate decrease in absolute tumor uptake. The versatile chemistry of these C-1 substituted bifunctional chelates provides a variety of possible enzyme cleavable moieties for further investigation.
研究了与传统双功能螯合剂(BC)和新型酶可代谢双功能螯合剂(BCM)偶联的¹¹¹In标记单克隆抗体(MoAb)的相关生物学特性。使用了一种针对小鼠B细胞淋巴瘤独特型的大鼠IgG2a MoAb。给 flank皮下组织患有B细胞淋巴瘤的小鼠静脉注射标记的MoAb,并在24小时或48小时进行成像或处死以进行器官计数。使用大鼠抗二硝基苯基IgG2a MoAb和非特异性多克隆小鼠IgG作为对照。与BC相比,使用BCM导致血液本底活性大幅降低、生物半衰期缩短以及肿瘤与血液比值增加,但绝对肿瘤摄取量适度降低。这些C-1取代的双功能螯合剂的多功能化学性质为进一步研究提供了多种可能的酶可裂解部分。