TY - JOUR
T1 - Development of Polar BODIPY-Tetrazines for Rapid Pretargeted Fluorescence Imaging
AU - Staudt, Markus
AU - Hvass, Lars
AU - Müller, Marius
AU - García-Vázquez, Rocío
AU - Jo Rgensen, Jesper Tranekjær
AU - Shalgunov, Vladimir
AU - Battisti, Umberto Maria
AU - Kjær, Andreas
AU - Herth, Matthias M
N1 - © 2024 The Authors. Published by American Chemical Society.
PY - 2024/10/15
Y1 - 2024/10/15
N2 - Polar BODIPY-tetrazine dyes were developed and clicked in vivo to a preaccumulated trans-cyclooctene-modified anti-TAG72 monoclonal antibody CC49 (CC49-TCO). The in vivo click performance was evaluated using an in-house developed ex vivo blocking assay. All tested polar BODIPY structures exhibited excellent in vivo binding, confirming that the turn-on tetrazine dyes successfully clicked in vivo to pretargeted CC49-TCO. Fluorescence imaging showed high tumor-to-muscle ratios of 4:1. This proof-of-concept study indicates that the pretargeting concept based on turn-on probes could be used for cancer treatments, such as photodynamic or -thermal therapy.
AB - Polar BODIPY-tetrazine dyes were developed and clicked in vivo to a preaccumulated trans-cyclooctene-modified anti-TAG72 monoclonal antibody CC49 (CC49-TCO). The in vivo click performance was evaluated using an in-house developed ex vivo blocking assay. All tested polar BODIPY structures exhibited excellent in vivo binding, confirming that the turn-on tetrazine dyes successfully clicked in vivo to pretargeted CC49-TCO. Fluorescence imaging showed high tumor-to-muscle ratios of 4:1. This proof-of-concept study indicates that the pretargeting concept based on turn-on probes could be used for cancer treatments, such as photodynamic or -thermal therapy.
UR - http://www.scopus.com/inward/record.url?scp=85205934300&partnerID=8YFLogxK
U2 - 10.1021/acsomega.4c06570
DO - 10.1021/acsomega.4c06570
M3 - Journal article
C2 - 39431101
SN - 2470-1343
VL - 9
SP - 42498
EP - 42505
JO - ACS omega
JF - ACS omega
IS - 41
ER -