Fast 18F Labeling of a Near-Infrared Fluorophore Enables Positron Emission Tomography and Optical Imaging of Sentinel Lymph Nodes

被引：74

作者：

Ting, Richard ^{[1
]}

Aguilera, Todd A. ^{[1
]}

Crisp, Jessica L. ^{[1
]}

Hall, David J. ^{[2
]}

Eckelman, William C. ^{[2
]}

Vera, David R. ^{[2
]}

Tsien, Roger Y. ^{[1
,3
]}

机构：

[1] Univ Calif San Diego, Dept Pharmacol 0647, La Jolla, CA 92093 USA

[2] Univ Calif San Diego, Dept Radiol, La Jolla, CA 92093 USA

[3] Univ Calif San Diego, Howard Hughes Med Inst, La Jolla, CA 92093 USA

来源：

BIOCONJUGATE CHEMISTRY | 2010年 / 21卷 / 10期

关键词：

IN-VIVO; PET; FLUORESCENT; STABILITY; PEPTIDES; DESIGN; BIOPSY; DYES;

D O I：

10.1021/bc1001328

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

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 F-18(-) 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 F-18 decay. This embodiment is superior to current SLN mapping agents such as nontargeted [Tc-99m]sulfur colloids and Isosulfan Blue, as well as the phase III targeted ligand [Tc-99m]SPECT Lymphoseek counterpart, species that are visible by SPECT or visible absorbance separately. Facile incorporation of F-18 into a NIRF probe should promote many synergistic PET and NIRF combinations.

引用

页码：1811 / 1819

页数：9

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