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Related Concept Videos

Affinity Chromatography01:03

Affinity Chromatography

Affinity chromatography is a powerful technique extensively utilized for separating and purifying specific biomolecules from complex mixtures. It capitalizes on the highly selective binding between an analyte and its counterpart, such as antibody-antigen interactions. The counterpart is immobilized on the stationary phase, forming an affinity column. The stationary phase typically consists of solid support, such as agarose or porous glass beads, immobilizing the affinity ligand. The mobile...

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Related Experiment Video

Updated: Jun 28, 2026

Harnessing the Bioorthogonal Inverse Electron Demand Diels-Alder Cycloaddition for Pretargeted PET Imaging
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Harnessing the Bioorthogonal Inverse Electron Demand Diels-Alder Cycloaddition for Pretargeted PET Imaging

Published on: February 3, 2015

Affinity-Tuned Albumin Hitchhiking Extends the Bioorthogonal Capture Window in Pretargeting Radiotheranostics.

Xie He1, Nicholas L Fletcher1,2, Gayathri R Ediriweera1,2

  • 1Australian Institute for Bioengineering and Nanotechnology and Centre for Advanced Imaging, University of Queensland, Brisbane, Queensland, Australia.

Advanced Healthcare Materials
|June 27, 2026
PubMed
Summary
This summary is machine-generated.

Albumin engagement prolongs radioligand circulation for improved pretargeted radiotheranostics. This strategy enhances tumor uptake and target-to-background ratios in PSMA-targeted systems.

Keywords:
albumin‐binding radioligandspretargetingprostate cancertargeted radiotheranosticstunable pharmacokinetics

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Published on: March 8, 2018

Area of Science:

  • Biomedical imaging
  • Radiopharmaceutical chemistry
  • Molecular imaging

Background:

  • Pretargeted radiotheranostics offer targeted delivery of radioactive payloads using in vivo click chemistry.
  • Suboptimal pharmacokinetics of small-molecule radioligands limit the in vivo reaction window and clinical translation.

Purpose of the Study:

  • To investigate an in situ albumin engagement strategy to improve radioligand pharmacokinetics.
  • To enhance the delivery of radioactive payloads in a PSMA-targeted pretargeting system.

Main Methods:

  • Incorporated an albumin binder into a clickable radioligand within a bispecific antibody pretargeting system.
  • Evaluated the effect of albumin binding on radioligand pharmacokinetics, tumor uptake, and target-to-background ratios.
  • Compared an albumin-binding construct (DOTA-mTz-sALB) with a non-albumin-binding construct.

Main Results:

  • Albumin engagement prolonged systemic circulation, expanding the bioorthogonal capture window without affecting target affinity.
  • Tumor-associated uptake increased ~3.5-fold (1.3% to 4.7% ID/g).
  • Tumor-to-liver ratios improved ~6-fold (0.1 to 0.6), with background clearance within 24-48 hours.

Conclusions:

  • Albumin engagement is a modular strategy to enhance pretargeted radiotheranostic delivery.
  • This approach improves pharmacokinetic properties and therapeutic efficacy.
  • The modular design allows independent optimization of radioligands and pretargeting agents for various receptor systems.