A modular platform for the rapid site-specific radiolabeling of proteins with 18F exemplified by quantitative positron emission tomography of human epidermal growth factor receptor 2.
作者： Herman S. Gill , Jeff N. Tinianow , Annie Ogasawara , Judith E. Flores , Alexander N. Vanderbilt
DOI: 10.1021/JM900420C
关键词:
摘要: Receptor-specific proteins produced by genetic engineering are attractive as PET imaging agents, but labeling with conventional (18)F-based prosthetic groups is problematic due to long synthesis times, poor radiochemical yields, and low specific activities. Therefore, we developed a modular platform for the rapid preparation of water-soluble capable efficiently introducing (18)F into proteins. The utility this demonstrated thiol-specific group, [(18)F]FPEGMA, which was used produce site-specifically (18)F-labeled protein ((18)F-trastuzumab-ThioFab) in 82 min total yield 13 +/- 3% activity 2.2 0.2 Ci/micromol. (18)F-trastuzumab-ThioFab retained biological native successfully validated vivo microPET Her2 expression xenograft tumor-bearing murine model modulated Hsp90 inhibitor, 17-(allylamino)-17-demethoxygeldanamycin.
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