SIB-DOTA: a trifunctional prosthetic group potentially amenable for multi-modal labeling that enhances tumor uptake of internalizing monoclonal antibodies

G Vaidyanathan, BJ White, DJ Affleck, XG Zhao…

Index: Vaidyanathan; White; Affleck; Zhao; Welsh; McDougald; Choi; Zalutsky Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 24 p. 6929 - 6939

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Citation Number: 7

Abstract

A major drawback of internalizing monoclonal antibodies (mAbs) radioiodinated with direct electrophilic approaches is that tumor retention of radioactivity is compromised by the rapid washout of iodo-tyrosine, the primary labeled catabolite for mAbs labeled via this strategy. In our continuing efforts to develop more versatile residualizing labels that could overcome this problem, we have designed SIB-DOTA, a prosthetic labeling template that combines the ...