通过2-亚氨基硫杂环戊烷将大环双功能螯合剂与抗体偶联的简化方法。
Simplified method for conjugating macrocyclic bifunctional chelating agents to antibodies via 2-iminothiolane.
作者信息
McCall M J, Diril H, Meares C F
机构信息
Chemistry Department, University of California, Davis 95616.
出版信息
Bioconjug Chem. 1990 May-Jun;1(3):222-6. doi: 10.1021/bc00003a007.
A one-step method for conjugating macrocyclic chelators to antibodies using the protein modification reagent 2-iminothiolane controls aggregation, maintains immunoreactivity, and produces consistent chelate/antibody ratios. Conjugation conditions have been investigated with the macrocyclic chelates 6-[p-(bromoacetamido)benzyl]-1,4,8,11-tetraazacyclotetradecane-N,N ',N",N"'-tetraacetic acid and 2-[p-(bromoacetamido)benzyl]-1,4,7,10-tetraazacyclododecane-N,N',N ",N"'-tetraacetic acid, with three different monoclonal antibodies. The bifunctional chelating agents are prepared by bromoacetylation of their amine precursors using a two-phase H2O/CHCl3 system, which improves product purity.
一种使用蛋白质修饰试剂2-亚氨基硫杂环戊烷将大环螯合剂与抗体偶联的一步法可控制聚集、维持免疫反应性并产生一致的螯合物/抗体比率。已使用大环螯合物6-[对-(溴乙酰氨基)苄基]-1,4,8,11-四氮杂环十四烷-N,N',N",N"'-四乙酸和2-[对-(溴乙酰氨基)苄基]-1,4,7,10-四氮杂环十二烷-N,N',N ",N"'-四乙酸与三种不同的单克隆抗体研究了偶联条件。双功能螯合剂通过使用两相H2O/CHCl3系统对其胺前体进行溴乙酰化制备，这提高了产物纯度。
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