211 At-labeled agents for alpha-immunotherapy: On the in vivo stability of astatine-agent bonds - Centre de recherche en cancérologie Nantes-Angers Unité Mixte de Recherche 892 Inserm - 6299 CNRS Accéder directement au contenu
Article Dans Une Revue European Journal of Medicinal Chemistry Année : 2016

211 At-labeled agents for alpha-immunotherapy: On the in vivo stability of astatine-agent bonds

Résumé

The application of 211 At to targeted cancer therapy is currently hindered by the rapid deastatination that occurs in vivo. As the deastatination mechanism is unknown, we tackled this issue from the viewpoint of the intrinsic properties of At-involving chemical bonds. An apparent correlation has been evidenced between in vivo stability of 211 At-labeled compounds and the AtÀR (R ¼ C, B) bond enthalpies obtained from relativistic quantum mechanical calculations. Furthermore, we highlight important differences in the nature of the AtÀC and AtÀB bonds of interest, e.g. the opposite signs of the effective astatine charges, which implies different stabilities with respect to the biological medium. Beyond their practical use for rationalizing the labeling protocols used for 211 At, the proposed computational approach can readily be used to investigate bioactive molecules labeled with other heavy radionuclides.
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Dates et versions

inserm-01414904 , version 1 (12-12-2016)

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Tahra F Ayed, Julien Pilmé, David Tézé, Fadel Bassal, Jacques F Barbet, et al.. 211 At-labeled agents for alpha-immunotherapy: On the in vivo stability of astatine-agent bonds. European Journal of Medicinal Chemistry, 2016, 116, pp.156 - 164. ⟨10.1016/j.ejmech.2016.03.082⟩. ⟨inserm-01414904⟩
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