Article ; Online: Design and characterization of fibroblast activation protein targeted pan-cancer imaging agent for fluorescence-guided surgery of solid tumors.
Journal of materials chemistry. B
2022 Volume 10, Issue 12, Page(s) 2038–2046
Abstract: Tumor-targeted fluorescent dyes have been shown to significantly improve a surgeon's ability to locate and resect occult malignant lesions, thereby enhancing a patient's chances of long term survival. Although several tumor-targeted fluorescent dyes have ...
Abstract | Tumor-targeted fluorescent dyes have been shown to significantly improve a surgeon's ability to locate and resect occult malignant lesions, thereby enhancing a patient's chances of long term survival. Although several tumor-targeted fluorescent dyes have been developed for imaging specific subsets of human cancers, no tumor-targeted dye has been designed that can image all cancer types. Based on observations that fibroblast activation protein (FAP) is upregulated on cancer-associated fibroblasts (CAFs) that infiltrate essentially all solid tumors, we have undertaken to develop a FAP-targeted fluorescent dye that can image CAFs without accumulating in healthy cells or fibroblasts. We report here that FTL-S-S0456, a novel FAP-targeted near infrared dye that binds FAP with high affinity (∼12 nM) and specificity (>5000-fold over PREP and DPP-IV), concentrates in all seven solid tumor types examined, yielding fluorescence images with high tumor to background ratios that persist for several days. We conclude that FTL-S-S0456 constitutes an excellent ligand-targeted near infrared dye that enables intra-operative imaging of most if not all solid tumors. |
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MeSH term(s) | Cell Line, Tumor ; Fibroblasts/metabolism ; Fluorescence ; Fluorescent Dyes/metabolism ; Humans ; Neoplasms/diagnostic imaging ; Neoplasms/surgery ; Proteins |
Chemical Substances | Fluorescent Dyes ; Proteins |
Language | English |
Publishing date | 2022-03-23 |
Publishing country | England |
Document type | Journal Article ; Research Support, Non-U.S. Gov't |
ZDB-ID | 2702241-9 |
ISSN | 2050-7518 ; 2050-750X |
ISSN (online) | 2050-7518 |
ISSN | 2050-750X |
DOI | 10.1039/d1tb02651h |
Database | MEDical Literature Analysis and Retrieval System OnLINE |
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