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High-Contrast Detection of Somatostatin Receptor Subtype‑2 for Fluorescence-Guided Surgery
Journal article   Open access   Peer reviewed

High-Contrast Detection of Somatostatin Receptor Subtype‑2 for Fluorescence-Guided Surgery

Servando Hernandez Vargas, Solmaz AghaAmiri, Sukhen C. Ghosh, Michael P. Luciano, Luis C. Borbon, Po Hien Ear, James R. Howe, Jennifer M. Bailey-Lundberg, Gregory D. Simonek, Daniel M. Halperin, …
Molecular pharmaceutics, Vol.19(11), pp.4241-4253
11/07/2022
DOI: 10.1021/acs.molpharmaceut.2c00583
PMCID: PMC9830638
PMID: 36174110
url
https://doi.org/10.1021/acs.molpharmaceut.2c00583View
Published (Version of record) Open Access

Abstract

Dye design can influence the ability of fluorescently labeled imaging agents to generate tumor contrast and has become an area of significant interest in the field of fluorescence-guided surgery (FGS). Here, we show that the charge-balanced near-infrared fluorescent (NIRF) dye FNIR-Tag enhances the imaging properties of a fluorescently labeled somatostatin analogue. In vitro studies showed that the optimized fluorescent conjugate MMC­(FNIR-Tag)-TOC bound primarily via somatostatin receptor subtype-2 (SSTR2), whereas its negatively charged counterpart with IRDye 800CW had higher off-target binding. NIRF imaging in cell line- and patient-derived xenograft models revealed markedly higher tumor contrast with MMC­(FNIR-Tag)-TOC, which was attributed to increased tumor specificity. Ex vivo staining of surgical biospecimens from primary and metastatic tumors, as well as involved lymph nodes, demonstrated binding to human tumors. Finally, in an orthotopic tumor model, a simulated clinical workflow highlighted our unique ability to use standard preoperative nuclear imaging for selecting patients likely to benefit from SSTR2-targeted FGS. Our findings demonstrate the translational potential of MMC­(FNIR-Tag)-TOC for intraoperative imaging and suggest broad utility for using FNIR-Tag in fluorescent probe development.
fluorescence-guided surgery somatostatin receptor dual labeling intraoperative imaging near-infrared fluorescence imaging cancer surgery

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