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Random and site-specific radiolabeling of [89Zr]Zr-DFO-anti-PD-L1-mAb iPET tracer

  • Yi-Ching Lin,
  • Chao-Wei Yang,
  • Shih-Chuan Tsai,
  • Shiou-Shiow Farn,
  • Fang-Yu Ou Yang,
  • Wei-Lin Lo,
  • Liang-Cheng Chen,
  • Kuo-Ting Chen,
  • Mao-Chi Weng,
  • Jui-Yin Kung,
  • Xin-Yu Qiu,
  • Ching-Chun Lu,
  • Feng-Yun J. Huang

摘要

Zirconium-89 radiolabeled immuno-positron emission tomography (89Zr-iPET) has become a critical tool for patient stratification before and after immunotherapies for therapeutic evaluation. In this study, random and site-specific radiolabeling of 89Zr-iPET tracers were investigated. Traditional lysine-based conjugation and enzyme-based GlyCLICK® kit method were used to prepare DFO-anti-PD-L1-mAb conjugates with a chelator-to-antibody ratio (CAR) of 0–7 and 2.0, respectively. Then, conjugates with different CAR levels were radiolabeled with 89Zr to obtain randomly or site-specifically radiolabeled 89Zr-iPET tracer.