文章基本信息

标题：Rapid and Selective Targeting of Heterogeneous Pancreatic Neuroendocrine Tumors
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作者：G. Kate Park ; Jeong Heon Lee ; Eduardo Soriano 等
期刊名称：iScience
印刷版ISSN：2589-0042
出版年度：2020
卷号：23
期号：4
页码：1-33
DOI：10.1016/j.isci.2020.101006
语种：English
出版社：Elsevier
摘要：SummaryDesign of tissue-specific contrast agents to delineate tumors from background tissues is a major unmet clinical need for ultimate surgical interventions. Bioconjugation of fluorophore(s) to a ligand has been mainly used to target overexpressed receptors on tumors. However, the size of the final targeted ligand can be large, >20 kDa, and cannot readily cross the microvasculature to meet the specific tissue, resulting in low targetability with a high background. Here, we report a small and hydrophilic phenoxazine with high targetability and retention to pancreatic neuroendocrine tumor. This bioengineered fluorophore permits sensitive detection of ultrasmall (<0.5 mm) ectopic tumors within a few seconds after a single bolus injection, highlighting every tumor in the pancreas from the surrounding healthy tissues with reasonable half-life. The knowledge-based approach and validation used to develop structure-inherent tumor-targeted fluorophores have a tremendous potential to improve treatment outcome by providing definite tumor margins for image-guided surgery.Graphical AbstractDisplay OmittedHighlights•Bioengineered near-infrared fluorescent small molecules for PNET imaging•Highlight tumors within a minute after a single bolus injection with improved retention•Sensitive and specific detection of ultrasmall ectopic tumors•Intraoperative image-guided navigation provides a surgical marginHistology; Chemistry; Cancer