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

被引：46

作者：

Gill, Herman S. ^{[1
]}

Tinianow, Jeff N. ^{[1
]}

Ogasawara, Annie ^{[1
]}

Flores, Judith E. ^{[1
]}

Vanderbilt, Alexander N. ^{[1
]}

Raab, Helga ^{[2
]}

Scheer, Justin M. ^{[2
]}

Vandlen, Richard ^{[2
]}

Williains, Simon-P. ^{[1
]}

Marik, Jan ^{[1
]}

机构：

[1] Genentech Inc, Dept Biomed Imaging, San Francisco, CA 94080 USA

[2] Genentech Inc, Dept Prot Chem, San Francisco, CA 94080 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 52卷 / 19期

关键词：

AZIDE-ALKYNE CYCLOADDITION; N-SUCCINIMIDYL; ANTIBODY FRAGMENTS; IMMUNO-PET; ANNEXIN-V; IN-VIVO; PEPTIDES; DEGRADATION; CONJUGATION; MALEIMIDE;

D O I：

10.1021/jm900420c

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

Receptor-specific proteins produced by genetic engineering are attractive as PET imaging agents, but labeling with conventional F-18-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 prosthetic groups capable of efficiently introducing F-18 into proteins. The utility of this platform is demonstrated by the thiol-specific prosthetic group, [F-18]FPEGMA, which was used to produce site-specifically F-18-labeled protein (F-18-trastuzumab-ThioFab) in 82 min with a total radiochemical yield of 13 +/- 3% and a specific activity of 2.2 +/- 0.2 Ci/mu mol. F-18-trastuzumab-ThioFab retained the biological activity of native protein and was successfully validated in vivo with microPET imaging of Her2 expression in a xenograft tumor-bearing murine model modulated by. the Hsp90 inhibitor, 17-(allylamino)-17-demethoxygeldanamycin.

引用

页码：5816 / 5825

页数：10

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