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Related Concept Videos

Imaging Studies II: Positron Emission Tomography and Scintigraphy01:25

Imaging Studies II: Positron Emission Tomography and Scintigraphy

Positron Emission Tomography (PET) is a medical imaging technique that provides crucial insights into the body's physiological functions at a molecular level. It is an indispensable resource for diagnosing, staging, and monitoring various illnesses, notably cancer, neurological disorders, and cardiovascular conditions.
Fundamental Principles of PET

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Development and Advantages of <i>O</i>-(Carboxymethyl)-<i>L</i>-tyrosine-Based PSMA-Targeting Theranostics for Prostate Cancer.

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Related Experiment Video

Updated: Jul 12, 2026

Automated Preparation of [68Ga]Ga-3BP-3940 on a Synthesis Module for PET Imaging of the Tumor Microenvironment
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Automated Preparation of [68Ga]Ga-3BP-3940 on a Synthesis Module for PET Imaging of the Tumor Microenvironment

Published on: April 25, 2025

Dual-Chelator conjugates for [68Ga]Ga- and [177Lu]Lu-based PSMA Radiotheranostics.

Wenbin Jin1, Yang Luo2, Zhaohui Zhu1

  • 1Department of Nuclear Medicine, Peking Union Medical College Hospital, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100875, China.

Bioorganic Chemistry
|July 10, 2026
PubMed
Summary

A novel dual-chelator strategy integrates diagnostic and therapeutic radioisotopes onto a single molecule targeting prostate cancer. This approach shows promise for advanced PSMA-targeted radiotheranostics, enhancing precision oncology.

Keywords:
Dual-chelatorPET imadingPSMARadioligands

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Pretargeted Radioimmunotherapy Based on the Inverse Electron Demand Diels-Alder Reaction
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Published on: January 29, 2019

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Pretargeted Radioimmunotherapy Based on the Inverse Electron Demand Diels-Alder Reaction
09:44

Pretargeted Radioimmunotherapy Based on the Inverse Electron Demand Diels-Alder Reaction

Published on: January 29, 2019

Area of Science:

  • Nuclear Medicine
  • Radiopharmaceutical Chemistry
  • Oncology

Background:

  • Prostate-specific membrane antigen (PSMA) is a key biomarker for prostate cancer (PCa).
  • Current PSMA-targeted radiotherapeutics often require separate imaging and therapeutic agents.
  • A unified platform for both diagnosis and therapy is desirable for improved precision medicine.

Purpose of the Study:

  • To develop and evaluate a novel dual-chelator strategy for PSMA-targeted radiotheranostics.
  • To create a single molecular platform capable of chelating both diagnostic (e.g., 68Ga) and therapeutic (e.g., 177Lu) radionuclides.
  • To assess the efficacy of these dual-chelator conjugates in vitro and in vivo for prostate cancer applications.

Main Methods:

  • Design and synthesis of three dual-chelator conjugates (PSMA-093 scaffold with HBED-CC and DOTA).
  • Radiolabeling with 68Ga (diagnostic) and 177Lu (therapeutic).
  • In vitro PSMA-binding affinity assays, cellular uptake studies, and in vivo PET/CT imaging and biodistribution studies in relevant models.

Main Results:

  • Successful radiolabeling of conjugates with 68Ga and 177Lu, with site-selective metal coordination confirmed by mass spectrometry.
  • Conjugates maintained high PSMA-binding affinity and showed enhanced cellular uptake in PSMA-overexpressing cells.
  • In vivo studies demonstrated favorable pharmacokinetics for the diagnostic agent ([68Ga]Ga-2) and high tumor uptake for the therapeutic agent ([177Lu]Lu-2).

Conclusions:

  • The dual-chelator strategy is a viable platform for developing next-generation PSMA-targeted radiotheranostic agents.
  • This approach allows for the integration of diagnostic and therapeutic functions within a single molecule, offering design flexibility.
  • The developed radiotheranostic agents show potential for effective tumor targeting and improved outcomes in prostate cancer treatment, advancing precision oncology.