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Advance in Radiochemistry, 2nd Edition
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Advance in Radiochemistry, 2nd Edition

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: 31 October 2025 | Viewed by 783

Special Issue Editor

Dr. Chang-Tong Yang

E-Mail Website
Guest Editor
1. Duke-NUS Medical School, 8 College Road, Singapore 169857, Singapore
2. Department of Nuclear Medicine and Molecular Imaging, Radiological Sciences Division, Singapore General Hospital, Outram Road, Singapore 169608, Singapore
Interests: radiochemistry and radiopharmaceuticals; radiolabeling techniques and radiosynthesis; production of radioisotopes; probe (radiotracer) development for nuclear imaging; theranostics of radiopharmaceuticals; radiation dose and safety
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Radiochemistry is a branch of chemistry that studies radiation from a molecular perspective and explores isotope transformation and radioactive reaction effects, a physical and medical property of radioisotopes. Research in radiochemistry is ongoing, with radioisotopes used to label chemical compounds such as radiopharmaceuticals (radiotracers) for drug development, involving radiopharmaceutical design and preparation, in vitro and in vivo biological studies, pharmacological study, and preclinical and clinical studies. 

This Special Issue will focus on the development of radiopharmaceuticals and their theranostic applications. Radiopharmaceuticals include all physicochemically characterized molecular structures such as small organic molecules, coordination compounds, and nanomaterials. The development of radiopharmaceuticals is devoted to (1) preparation of precursors; (2) radiolabeling techniques including radiosynthesis, purification, and analysis; (3) in vitro and in vivo radiopharmaceutical research and pharmacological investigation; (4) radiotracers for PET/SPECT imaging, preclinical trials, diagnostic and therapeutic applications, and potential personalized medicine.

Dr. Chang-Tong Yang
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • radiochemistry
  • radionuclide (radioisotopes)
  • radiolabeling
  • radiopharmaceutical (radiotracer)
  • nuclear medicine
  • theranostics (diagnostics and therapeutics)
  • molecular imaging

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Related Special Issue

Published Papers (2 papers)

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Research

17 pages, 2255 KiB  
Article
Engineering a Radiohybrid PSMA Ligand with an Albumin-Binding Moiety and Pharmacokinetic Modulation via an Albumin-Binding Competitor for Radiotheranostics
by Saki Hirata, Hiroaki Echigo, Masayuki Munekane, Kenji Mishiro, Kohshin Washiyama, Takeshi Fuchigami, Hiroshi Wakabayashi, Kazuhiro Takahashi, Seigo Kinuya and Kazuma Ogawa
Molecules 2025, 30(13), 2804; https://doi.org/10.3390/molecules30132804 - 29 Jun 2025
Viewed by 123
Abstract
The prostate-specific membrane antigen (PSMA) is a well-established target for radiotheranostics in prostate cancer. We previously demonstrated that 4-(p-astatophenyl)butyric acid (APBA), an albumin-binding moiety (ABM) labeled with astatine-211 (211At), enables the modulation of pharmacokinetics and enhancement of therapeutic efficacy [...] Read more.
The prostate-specific membrane antigen (PSMA) is a well-established target for radiotheranostics in prostate cancer. We previously demonstrated that 4-(p-astatophenyl)butyric acid (APBA), an albumin-binding moiety (ABM) labeled with astatine-211 (211At), enables the modulation of pharmacokinetics and enhancement of therapeutic efficacy when combined with the post-administration of an albumin-binding competitor. However, this strategy has not been explored in PSMA-targeting ligands. We designed and synthesized [211At]6, a novel PSMA ligand structurally analogous to PSMA-617 with APBA. The compound was obtained via a tin–halogen exchange reaction from the corresponding tributylstannyl precursor. Comparative cellular uptake and biodistribution studies were conducted with [211At]6, its radioiodinated analog [125I]5, and [67Ga]Ga-PSMA-617. To assess pharmacokinetic modulation, sodium 4-(p-iodophenyl)butanoate (IPBA), an albumin-binding competitor, was administered 1 h postinjection of [125I]5 and [211At]6 at a 10-fold molar excess relative to blood albumin. The synthesis of [211At]6 gave a radiochemical yield of 15.9 ± 7.7% and a radiochemical purity > 97%. The synthesized [211At]6 exhibited time-dependent cellular uptake and internalization, with higher uptake levels than [67Ga]Ga-PSMA-617. Biodistribution studies of [211At]6 in normal mice revealed a prolonged blood retention similar to those of [125I]5. Notably, post-administration of IPBA significantly reduced blood radioactivity and non-target tissue accumulation of [125I]5 and [211At]6. We found that ABM-mediated pharmacokinetic control was applicable to PSMA-targeted radiotherapeutics, broadening its potential for the optimization of radiotheranostics. Full article
(This article belongs to the Special Issue Advance in Radiochemistry, 2nd Edition)
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11 pages, 1309 KiB  
Article
Cytotoxicity Comparison of 99mTc-Labeled Peptide Antagonist and Agonist Targeting the SSTR2 Receptor in AR42J Cells
by Sahar Nosrati Shanjani, Monika Łyczko, Rafał Walczak, Przemysław Koźmiński, Emilia Majka, Jerzy Narbutt, Wioletta Wojdowska, Agnieszka Majkowska-Pilip and Aleksander Bilewicz
Molecules 2025, 30(8), 1715; https://doi.org/10.3390/molecules30081715 - 11 Apr 2025
Viewed by 485
Abstract
Auger electrons are low-energy, high-linear-energy-transfer particles that deposit their energy over nanometers distances. Their biological impact depends heavily on where the radionuclide is localized within the cell. To verify the hypothesis that the cell membrane may be a better molecular target than the [...] Read more.
Auger electrons are low-energy, high-linear-energy-transfer particles that deposit their energy over nanometers distances. Their biological impact depends heavily on where the radionuclide is localized within the cell. To verify the hypothesis that the cell membrane may be a better molecular target than the cytoplasm in Auger electron therapy, we investigated whether the radiotoxicity of 99mTc varied depending on its location in the cell. The behavior of peptide radiopharmaceuticals 99mTc-TECANT-1 targeted the cell membrane was compared with 99mTc-TEKTROTYD directed to the cytoplasm. Our findings confirmed that 99mTc-TECANT-1 displayed greater binding to AR-42-J cells than 99mTc-TEKTROTYD. Additionally, it was demonstrated that the receptor agonist 99mTc-TEKTROTYD is localized in more than 90% of the cytoplasm, while 99mTc-TECANT-1 is found in 60–80% of the cell membrane. When evaluating cell survival using the MTS assay, we observed that toxicity was significantly higher when 99mTc was targeted to the membrane compared to the cytoplasm. This indicates that, for 99mTc, as with 161Tb, the membrane is a more sensitive target for Auger electrons than the cytoplasm. Our results also suggest that receptor antagonists labelled with therapeutic doses of 99mTc may be effective in treating certain cancers. However, further detailed studies, particularly dosimetric investigations, are necessary to validate these findings. Full article
(This article belongs to the Special Issue Advance in Radiochemistry, 2nd Edition)
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