Near-Infrared-Emitting BODIPY-trisDOTA111In as a Monomolecular Multifunctional Imaging Probe: From Synthesis to In Vivo Investigations

Authors:

Dr. Nicolas Maindron, Dr. Martin Ipuy, Dr. Claire Bernhard,Dr. Damien Lhenry, Dr. Mathieu Moreau, Dr. Sabin Carme, Dr. Alexandra Oudot, Dr. Bertrand Collin, Dr. Jean-Marc Vrigneaud, Dr. Peggy Provent, Prof. François Brunotte, Prof. Franck Denat, Dr. Christine Goze

Abstract:

A new generation of monomolecular imaging probes (MOMIP) based on a distyryl-BODIPY (BODIPY=boron-dipyrromethene) coupled with three DOTA macrocycles has been prepared (DOTA=1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid). The MOMIP presents good fluorescence properties and is very stable in serum. The bimodal probe was conjugated to trastuzumab, and an optical in vivo study showed high accumulation of the imaging agent at the tumor site. (111) In radiometallation of the bioconjugate was performed in high radiochemical yield, highlighting the potential of this new BODIPY-chelators derivative as a bimodal imaging probe.

Ref: Chemistry. 2016 Aug 26; 22(36):12670-4. doi: 10.1002/chem.201602886. Epub 2016 Aug 2.

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