Simplified Method for Conjugating Macrocyclic Bifunctional Chelating Agents to Antibodies via 2-Iminothiolane

  • McCall M
  • Diril H
  • Meares C
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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 che-lates 6-[ p -(bromoacetamido) benzyl] -1,4,8,1 l-tetraazacyclotetradecane-N,N',N",N"'-tetraacetic acid and 2-[p-(bromoacetamido) ben~yl]",4,7,10-tetraazacyclododecane-N,N',N",N'"-tetraacetic acid, with three different monoclonal antibodies. The bifunctional chelating agents are prepared by bromoacetyla-tion of their amine precursors using a two-phase HZO/CHC13 system, which improves product purity. The attachment of metal ions to monoclonal antibod-ies (mAbs)l for medical applications demands extreme stability under physiological conditions, with no signifi-cant release of metal (1-4). Development of antibody-macrocyclic chelate conjugates for tumor localization and therapy has led to the following improvements. In our earliest study of the conjugate of 6-[p-(bromoacetamido) benzyl]-1,4,8,1 l-tetraazacyclotetrade-cane-N,NI,N",N"'-tetraacetic acid (BAT) with the mouse

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  • Michael J. McCall

  • Habibe Diril

  • Claude F. Meares

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