Design, synthesis, and biological evaluation of a multifunctional neuropeptide-Y conjugate for selective nuclear delivery of radiolanthanides
作者: Adrien ChastelDennis J. WormIsabel D. AlvesDelphine VimontMelina PetrelSamantha FernandezPhilippe GarriguePhilippe FernandezElif HindiéAnnette G. Beck-SickingerClément Morgat
作者单位: 1Department of Nuclear Medicine, University Hospital of Bordeaux, F-33076, Bordeaux, France
2University of Bordeaux, INCIA UMR 5287, F-33400, Talence, France
3CNRS, INCIA UMR 5287, F-33400, Talence, France
4Institute of Biochemistry, Faculty of Life Sciences, Leipzig University, Brüderstr. 34, 04103, Leipzig, Germany
5Institute of Chemistry & Biology of Membranes & Nano-objects (CBMN), CNRS UMR 5248, University of Bordeaux, F-33600, Pessac, France
6University of Bordeaux, Bordeaux Imaging Center, F-33000, Bordeaux, France
7Aix-Marseille University, INSERM, Institut National de la Recherche Agronomique, Centre de Recherche en Cardiovasculaire et Nutrition, 13385, Marseille, France
8Aix-Marseille University, Centre Européen de Recherche en Imagerie Médicale, 13005, Marseille, France
刊名: EJNMMI Research, 2020, Vol.10 (1), pp.125-135
来源数据库: Springer Nature Journal
DOI: 10.1186/s13550-020-0612-8
关键词: 161TbNeuropeptide-YSub-cellular deliveryAuger-emitterBreast cancer
英文摘要: Abstract(#br)Background(#br)Targeting G protein-coupled receptors on the surface of cancer cells with peptide ligands is a promising concept for the selective tumor delivery of therapeutically active cargos, including radiometals for targeted radionuclide therapy (TRT). Recently, the radiolanthanide terbium-161 (161Tb) gained significant interest for TRT application, since it decays with medium-energy β-radiation but also emits a significant amount of conversion and Auger electrons with short tissue penetration range. The therapeutic efficiency of radiometals emitting Auger electrons, like 161Tb, can therefore be highly boosted by an additional subcellular delivery into the nucleus, in order to facilitate maximum dose deposition to the DNA. In this study, we describe...
全文获取路径: Springer Nature  (合作)