18F-Based Pretargeted PET Imaging Based on Bioorthogonal Diels–Alder Click Chemistry

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• 作者：Jan-Philip Meyer ; Jacob L. Houghton ; Paul Kozlowski ; Dalya Abdel-Atti ; Thomas Reiner ; Naga Vara Kishore Pillarsetty ; Wolfgang W. Scholz ; Brian M. Zeglis ; Jason S. Lewis
• 刊名：Bioconjugate Chemistry
• 出版年：2016
• 出版时间：February 17, 2016
• 年：2016
• 卷：27
• 期：2
• 页码：298-301
• 全文大小：273K
• ISSN：1520-4812

文摘

A first-of-its-kind ¹⁸F pretargeted PET imaging approach based on the bioorthogonal inverse electron demand Diels–Alder (IEDDA) reaction between tetrazine (Tz) and trans-cyclooctene (TCO) is presented. As proof-of-principle, a TCO-bearing immunoconjugate of the anti-CA19.9 antibody 5B1 and an Al[¹⁸F]NOTA-labeled tetrazine radioligand were harnessed for the visualization of CA19.9-expressing BxPC3 pancreatic cancer xenografts. Biodistribution and ¹⁸F-PET imaging data clearly demonstrate that this methodology effectively delineates tumor mass with activity concentrations up to 6.4 %ID/g at 4 h after injection of the radioligand.