2025-08-07 北海道大学
短波赤外蛍光色素が結合した抗がん剤であるタモキシフェン
<関連情報>
- https://www.hokudai.ac.jp/news/2025/08/post-2005.html
- https://www.hokudai.ac.jp/news/pdf/250807_pr2.pdf
- https://pubs.acs.org/doi/10.1021/acsmedchemlett.5c00310
エトロゲン受容体標的がんイメージングのための短波赤外(SWIR)発光タモキシフェン結合シアニン色素 Shortwave Infrared (SWIR)-Emitting Tamoxifen-Conjugated Cyanine Dyes for Estrogen Receptor-Targeted Cancer Imaging
Aravind Kanda Swamy,Mahadeva M. M. Swamy,Kohei Yuyama,Takeshi Jin,and Kenji Monde
ACS Medicinal Chemistry Letters Published: July 18, 2025
DOI:https://doi.org/10.1021/acsmedchemlett.5c00310
Abstract
Fluorescence-guided tumor detection using tumor-targeting imaging agents is critical for achieving complete surgical resection with tumor-free margins. Shortwave infrared (SWIR, 900–1400 nm) fluorescence imaging enables deeper tissue penetration due to reduced tissue autofluorescence and scattering relative to conventional visible (400–700 nm) and near-infrared (NIR, 700–900 nm) imaging. In this study, a series of estrogen receptor (ER)-targeting imaging probes were developed by conjugating the anticancer drug-based ligand tamoxifen (TAM) with the FDA-approved indocyanine green (ICG), yielding ICG-TAM and its π-conjugated extended analogues, ICG-C9-TAM and ICG-C11-TAM. Although ICG-TAM exhibits peak absorption and emission in the NIR region, it also emits in the SWIR region. ICG-C9-TAM and ICG-C11-TAM were further evaluated for noninvasive SWIR fluorescence imaging. SWIR fluorescence imaging was performed in ER-expressing cervical and breast cancer cells using the TAM conjugates. These findings support the use of receptor-targeted ligands for specific biomolecular imaging in ER-positive cancer models.
