Dokument-ID Dokumenttyp Autoren/innen Persönliche Herausgeber/innen Haupttitel Abstract Auflage Verlagsort Verlag Herausgeber (Institution) Erscheinungsjahr Titel des übergeordneten Werkes Jahrgang/Band ISBN Veranstaltung Veranstaltungsort Beginndatum der Veranstaltung Enddatum der Veranstaltung Ausgabe/Heft Erste Seite Letzte Seite URN DOI Lizenz Datum der Freischaltung OPUS4-53731 Vortrag Resch-Genger, Ute; Wegner, Karl David; Kalot, G.; Busser, B.; Pliquett, J.; Köster, U.; Koll, J. C.; Denat, F.; Bodio, E.; Goze, C.; Sacey, L. NIR aza-BODIPY: a new vector for boron neutron capture therapy (BNCT) Boron neutron capture therapy (BNCT) relies on the activation of 10B by thermal neutrons, which results in small highly energetic particle emission inducing cancer cells damage. However, in order to overcome the limits of the currently used BNCT agents, it is necessary to design new systems, which can specifically accumulate and deliver a sufficient amount of 10B in tumors. In this study, we designed a 10B-BSH-containing aza-BODIPY (aza-SWIR-BSH). It enabled the efficient vectorization of clinically used 10B-BSH to the tumor, resulting in higher therapeutic activity than the 10B-BSH alone. 2021 EMIM 2021 Göttingen, Germany 24.08.2021 28.08.2021 2021-11-11 OPUS4-51228 Zeitschriftenartikel Kalot, G.; Godard, A.; Busser, B.; Pliquett, J.; Broekgaarden, M.; Motto-Ros, V.; Wegner, Karl David; Resch-Genger, Ute; Köster, U.; Denat, F.; Coll, J.-L.; Bodio, E.; Goze, C.; Sancey, L. Aza-BODIPY: A New Vector for Enhanced Theranostic Boron Neutron Capture Therapy Applications Boron neutron capture therapy (BNCT) is a radiotherapeutic modality based on the nuclear capture of slow neutrons by stable 10B atoms followed by charged particle Emission that inducing extensive damage on a very localized level (<10 um). To be effcient, a suffcient amount of 10B should accumulate in the tumor area while being almost cleared from the normal surroundings. A water-soluble aza-boron-dipyrromethene dyes (BODIPY) fluorophore was reported to strongly accumulate in the tumor area with high and BNCT compatible Tumor/Healthy Tissue ratios. The clinically used 10B-BSH (sodium borocaptate) was coupled to the water-soluble aza-BODIPY platform for enhanced 10B-BSH tumor vectorization. We demonstrated a strong uptake of the compound in tumor cells and determined its biodistribution in mice-bearing tumors. A model of chorioallantoic membrane-bearing glioblastoma xenograft was developed to evidence the BNCT potential of such compound, by subjecting it to slow neutrons. We demonstrated the Tumor accumulation of the compound in real-time using optical imaging and ex vivo using elemental imaging based on laser-induced breakdown spectroscopy. The tumor growth was significantly reduced as compared to BNCT with 10B-BSH. Altogether, the fluorescent aza-BODIPY/10B-BSH compound is able to vectorize and image the 10B-BSH in the tumor area, increasing its theranostic potential for effcient approach of BNCT. MDPI 2020 Cells 9 9 1953 urn:nbn:de:kobv:b43-512280 10.3390/cells9091953 https://creativecommons.org/licenses/by/4.0/deed.de 2020-09-16 OPUS4-50695 Zeitschriftenartikel Godard, A.; Kalot, G.; Pliquett, J.; Busser, B.; Le Guével, X.; Wegner, Karl David; Resch-Genger, Ute; Russelin, Y.; Coll, J.-L.; Denat, F.; Bodio, E.; Goze, C.; Sancey, L. Water-Soluble Aza-BODIPYs: Biocompatible Organic Dyes for High Contrast In Vivo NIR-II Imaging A simple NIR-II emitting water-soluble system has been developed and applied in vitro and in vivo. In vitro, the fluorophore quickly accumulated in 2D and 3D cell cultures and rapidly reached the tumor in rodents, showing high NIR-II contrast for up to 1 week. This very efficient probe possesses all the qualities necessary for translation to the clinic as well as for the development of NIR-II emitting materials. ACS Publications 2020 Bioconjugate Chemistry 31 4 1088 1092 10.1021/acs.bioconjchem.0c00175 2020-04-27 OPUS4-57293 Zeitschriftenartikel Godard, A.; Kalot, G.; Privat, M.; Bendellaa, M.; Busser, B.; Wegner, Karl David; Denat, F.; Le Guevel, X.; Coll, J.-L.; Paul, C.; Bodio, E.; Goze, C.; Sancey, L. NIR-II Aza-BODIPY Dyes Bioconjugated to Monoclonal Antibody Trastuzumab for Selective Imaging of HER2-Positive Ovarian Cancer Using fluorescence-guided surgery (FGS) to cytoreductive surgery helps achieving complete resection of microscopic ovarian tumors. The use of visible and NIR-I fluorophores has led to beneficial results in clinical trials; however, involving NIR-II dyes seems to outperform those benefits due to the deeper tissue imaging and higher signal/noise ratio attained within the NIR-II optical window. In this context, we developed NIR-II emitting dyes targeting human epidermal growth factor receptor 2 (HER2)-positive ovarian tumors by coupling water-soluble NIR-II aza-BODIPY dyes to the FDA-approved anti-HER2 antibody, namely, trastuzumab. These bioconjugated NIR-II-emitting dyes displayed a prolonged stability in serum and a maintained affinity toward HER2 in vitro. We obtained selective targeting of HER2 positive tumors (SKOV-3) in vivo, with a favorable tumor accumulation. We demonstrated the fluorescence properties and the specific HER2 binding of the bioconjugated dyes in vivo and thus their potential for NIR-II FGS in the cancer setting. ACS Publications 2023 Journal of Medicinal Chemistry 66 7 5185 5195 10.1021/acs.jmedchem.3c00100 2023-04-13 OPUS4-59607 Zeitschriftenartikel Chazeau, E.; Fabre, C.; Privat, M.; Godard, A.; Racoeur, C.; Bodio, E.; Busser, B.; Wegner, Karl David; Sancey, L.; Paul, C.; Goze, C. Comparison of the In Vitro and In Vivo Behavior of a Series of NIR-II-Emitting Aza-BODIPYs Containing Different Water-Solubilizing Groups and Their Trastuzumab Antibody Conjugates The development of new fluorescent organic probes effective in the NIR-II region is currently a fast-growing field and represents a challenge in the domain of medical imaging. In this study, we have designed and synthesized an innovative series of aza-boron dipyrromethenes emitting in the NIR-II region. We have investigated the effect of different water-solubilizing groups not only on the photophysical properties of the compounds but also on their in vitro and in vivo performance after bioconjugation to the antibody trastuzumab. Remarkably, we discovered that the most lipophilic compound unexpectedly displayed the most favorable in vivo properties after bioconjugation. This underlines the profound influence that the fluorophore functionalization approach can have on the efficiency of the resulting imaging agent. ACS Publications 2024 Journal of Medicinal Chemistry 1 13 10.1021/acs.jmedchem.3c02139 2024-03-06