Skip to Main content Skip to Navigation
Journal articles

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

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.
Document type :
Journal articles
Complete list of metadatas

Cited literature [69 references]  Display  Hide  Download

https://www.hal.inserm.fr/inserm-01414904
Contributor : Elizabeth Bernardo <>
Submitted on : Monday, December 12, 2016 - 4:33:30 PM
Last modification on : Friday, November 6, 2020 - 11:34:26 AM
Long-term archiving on: : Tuesday, March 28, 2017 - 12:36:53 AM

File

 Restricted access
To satisfy the distribution rights of the publisher, the document is embargoed until : jamais

Please log in to resquest access to the document

Identifiers

Citation

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

Share

Metrics

Record views

508