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

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

doi:10.1021/acs.bioconjchem.5b00504

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

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

Radiology

Memorial Sloan-Kettering Cancer Center
MabVax Therapeutics
City University of New York

Research output: Contribution to journal › Article › peer-review

153 Scopus citations

Abstract

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.

Original language	English
Pages (from-to)	298-301
Number of pages	4
Journal	Bioconjugate Chemistry
Volume	27
Issue number	2
DOIs	https://doi.org/10.1021/acs.bioconjchem.5b00504
State	Published - Feb 17 2016

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title = "18F-Based Pretargeted PET Imaging Based on Bioorthogonal Diels-Alder Click Chemistry",

abstract = "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.",

author = "Meyer, \{Jan Philip\} and Houghton, \{Jacob L.\} and Paul Kozlowski and Dalya Abdel-Atti and Thomas Reiner and Pillarsetty, \{Naga Vara Kishore\} and Scholz, \{Wolfgang W.\} and Zeglis, \{Brian M.\} and Lewis, \{Jason S.\}",

note = "Publisher Copyright: {\textcopyright} 2015 American Chemical Society.",

year = "2016",

month = feb,

day = "17",

doi = "10.1021/acs.bioconjchem.5b00504",

language = "English",

volume = "27",

pages = "298--301",

journal = "Bioconjugate Chemistry",

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T1 - 18F-Based Pretargeted PET Imaging Based on Bioorthogonal Diels-Alder Click Chemistry

AU - Meyer, Jan Philip

AU - Houghton, Jacob L.

AU - Kozlowski, Paul

AU - Abdel-Atti, Dalya

AU - Reiner, Thomas

AU - Pillarsetty, Naga Vara Kishore

AU - Scholz, Wolfgang W.

AU - Zeglis, Brian M.

AU - Lewis, Jason S.

PY - 2016/2/17

Y1 - 2016/2/17

N2 - 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.

AB - 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.

UR - https://www.scopus.com/pages/publications/84959449467

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DO - 10.1021/acs.bioconjchem.5b00504

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JO - Bioconjugate Chemistry

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IS - 2

ER -

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

Abstract

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