211 At-labeled agents for alpha-immunotherapy: On the in vivo stability of astatine-agent bonds - Archive ouverte HAL Access content directly
Journal Articles European Journal of Medicinal Chemistry Year : 2016

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

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Abstract

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 and 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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