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Apr 1 – 5, 2019
Fairmont Château Laurier Hotel
UTC timezone

Bioconjugation of actinides using a peptoid scaffold

Not scheduled
Fairmont Château Laurier Hotel

Fairmont Château Laurier Hotel


Dr Julian Rees (Lawrence Berkeley National Lab)


The targeted delivery of alpha-generating radionuclides such as actinium-225 and thorium-227 is emerging as a promising treatment approach for a range of cancers. Advances in protein engineering are driving new developments in targeted drug delivery through increased availability of monoclonal antibodies and similar delivery vehicles. This work utilizes a modular, solid-phase synthetic method to generate biopolymers suitable for chelating f-block elements. The peptoid platform, polymeric chains of N-substituted glycines, can incorporate essentially any functional group bearing a pendant primary amine, allowing us prepare a tetramer of 1,2-hydroxypyridinone (HOPO) moieties optimized for actinide chelation. Further inclusion of a range of suitable functionalities enables bioconjugation via maleimide-Cys, succinate ester-Lys, or azide-alkyne coupling chemistry. Antibody-peptoid conjugates provide a versatile platform for antigen-specific delivery of therapeutic alpha generators, as well as other radionuclides such as zirconium-89, a positron emitter ideally suited for PET imaging.
Funding Agency United States Department of Energy
Email Address
Presentation Type Poster

Primary author

Dr Julian Rees (Lawrence Berkeley National Lab)


Prof. Rebecca Abergel (University of California, Berkeley)

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