Fast 18F labeling of a near-infrared fluorophore enables positron emission tomography and optical imaging of sentinel lymph nodes

Richard Ting; Todd A. Aguilera; Jessica L. Crisp; David J. Hall; William C. Eckelman; David R. Vera; Roger Y. Tsien

doi:10.1021/bc1001328

Fast ¹⁸F labeling of a near-infrared fluorophore enables positron emission tomography and optical imaging of sentinel lymph nodes

Richard Ting, Todd A. Aguilera, Jessica L. Crisp, David J. Hall, William C. Eckelman, David R. Vera, Roger Y. Tsien

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

77 Scopus citations

Abstract

We combine a novel boronate trap for F^- with a near-infrared fluorophore into a single molecule. Attachment to targeting ligands enables localization by positron emission tomography (PET) and near-infrared fluorescence (NIRF). Our first application of this generic tag is to label Lymphoseek (tilmanocept), an agent designed for receptor-specific sentinel lymph node (SLN) mapping. The new conjugate incorporates ¹⁸F^- in a single, aqueous step, targets mouse SLN rapidly (1 h) with reduced distal lymph node accumulation, permits PET or scintigraphic imaging of SLN, and enables NIRF-guided excision and histological verification even after ¹⁸F decay. This embodiment is superior to current SLN mapping agents such as nontargeted [^99mTc]sulfur colloids and Isosulfan Blue, as well as the phase III targeted ligand [^99mTc]SPECT Lymphoseek counterpart, species that are visible by SPECT or visible absorbance separately. Facile incorporation of ¹⁸F into a NIRF probe should promote many synergistic PET and NIRF combinations.

Original language	English (US)
Pages (from-to)	1811-1819
Number of pages	9
Journal	Bioconjugate Chemistry
Volume	21
Issue number	10
DOIs	https://doi.org/10.1021/bc1001328
State	Published - Oct 20 2010

ASJC Scopus subject areas

Biotechnology
Bioengineering
Biomedical Engineering
Pharmacology
Pharmaceutical Science
Organic Chemistry

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title = "Fast 18F labeling of a near-infrared fluorophore enables positron emission tomography and optical imaging of sentinel lymph nodes",

abstract = "We combine a novel boronate trap for F- with a near-infrared fluorophore into a single molecule. Attachment to targeting ligands enables localization by positron emission tomography (PET) and near-infrared fluorescence (NIRF). Our first application of this generic tag is to label Lymphoseek (tilmanocept), an agent designed for receptor-specific sentinel lymph node (SLN) mapping. The new conjugate incorporates 18F- in a single, aqueous step, targets mouse SLN rapidly (1 h) with reduced distal lymph node accumulation, permits PET or scintigraphic imaging of SLN, and enables NIRF-guided excision and histological verification even after 18F decay. This embodiment is superior to current SLN mapping agents such as nontargeted [99mTc]sulfur colloids and Isosulfan Blue, as well as the phase III targeted ligand [99mTc]SPECT Lymphoseek counterpart, species that are visible by SPECT or visible absorbance separately. Facile incorporation of 18F into a NIRF probe should promote many synergistic PET and NIRF combinations.",

author = "Richard Ting and Aguilera, {Todd A.} and Crisp, {Jessica L.} and Hall, {David J.} and Eckelman, {William C.} and Vera, {David R.} and Tsien, {Roger Y.}",

year = "2010",

month = oct,

day = "20",

doi = "10.1021/bc1001328",

language = "English (US)",

volume = "21",

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TY - JOUR

T1 - Fast 18F labeling of a near-infrared fluorophore enables positron emission tomography and optical imaging of sentinel lymph nodes

AU - Ting, Richard

AU - Aguilera, Todd A.

AU - Crisp, Jessica L.

AU - Hall, David J.

AU - Eckelman, William C.

AU - Vera, David R.

AU - Tsien, Roger Y.

PY - 2010/10/20

Y1 - 2010/10/20

N2 - We combine a novel boronate trap for F- with a near-infrared fluorophore into a single molecule. Attachment to targeting ligands enables localization by positron emission tomography (PET) and near-infrared fluorescence (NIRF). Our first application of this generic tag is to label Lymphoseek (tilmanocept), an agent designed for receptor-specific sentinel lymph node (SLN) mapping. The new conjugate incorporates 18F- in a single, aqueous step, targets mouse SLN rapidly (1 h) with reduced distal lymph node accumulation, permits PET or scintigraphic imaging of SLN, and enables NIRF-guided excision and histological verification even after 18F decay. This embodiment is superior to current SLN mapping agents such as nontargeted [99mTc]sulfur colloids and Isosulfan Blue, as well as the phase III targeted ligand [99mTc]SPECT Lymphoseek counterpart, species that are visible by SPECT or visible absorbance separately. Facile incorporation of 18F into a NIRF probe should promote many synergistic PET and NIRF combinations.

AB - We combine a novel boronate trap for F- with a near-infrared fluorophore into a single molecule. Attachment to targeting ligands enables localization by positron emission tomography (PET) and near-infrared fluorescence (NIRF). Our first application of this generic tag is to label Lymphoseek (tilmanocept), an agent designed for receptor-specific sentinel lymph node (SLN) mapping. The new conjugate incorporates 18F- in a single, aqueous step, targets mouse SLN rapidly (1 h) with reduced distal lymph node accumulation, permits PET or scintigraphic imaging of SLN, and enables NIRF-guided excision and histological verification even after 18F decay. This embodiment is superior to current SLN mapping agents such as nontargeted [99mTc]sulfur colloids and Isosulfan Blue, as well as the phase III targeted ligand [99mTc]SPECT Lymphoseek counterpart, species that are visible by SPECT or visible absorbance separately. Facile incorporation of 18F into a NIRF probe should promote many synergistic PET and NIRF combinations.

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JO - Bioconjugate Chemistry

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Fast ¹⁸F labeling of a near-infrared fluorophore enables positron emission tomography and optical imaging of sentinel lymph nodes

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