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Targeted Radionuclide Diagnosis and Therapy of Prostate Cancer—From Basic Research...
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Targeted Radionuclide Diagnosis and Therapy of Prostate Cancer—From Basic Research to Clinical Perspectives

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

Deadline for manuscript submissions: closed (31 October 2023) | Viewed by 18123

Special Issue Editor

Prof. Dr. Anna Lankoff

E-Mail Website
Guest Editor
1. Centre for Radiobiology and Biological Dosimetry, Institute of Nuclear Chemistry and Technology, Dorodna 16, 03-195 Warsaw, Poland
2. Department of Medical Biology, Institute of Biology, Jan Kochanowski University, Uniwersytecka 7, 24-406 Kielce, Poland
Interests: radiobiology; molecular biology; genetics; radiation-induced DNA damage and repair; cancer; biomarkers; radiopharmaceuticals for targeted cancer therapy

Special Issue Information

Dear Colleagues,

It is a pleasure to invite you to submit a manuscript to this Special Issue of Molecules, entitled Targeted Radionuclide Diagnosis and Therapy of Prostate Cancer—From Basic Research to Clinical Perspectives.

Prostate cancer is the most commonly diagnosed malignancy in men and the second leading cause of cancer-related death. Due to the significant mortality and morbidity rate associated with the progression of this disease, there is an urgent need for the development and application of precise diagnostic imaging agents and effective therapeutic strategies for prostate cancer patients. In recent years, tremendous progress has been made in managing prostate cancer patients, partially due to achievements in radioligand-driven imaging and therapy. This Special Issue welcomes original research articles, communications and review articles dealing with the design, synthesis, and evaluation of new potentially active radiopharmaceuticals for the radionuclide-targeted diagnosis and therapy of prostate cancer. Studies using pre- and clinical data on radiotheranostics and nanoparticle-based radiopharmaceutical applications in prostate cancer diagnosis and therapy, including their safety and efficacy, are also welcome.

Prof. Dr. Anna Lankoff
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

  • prostate cancer
  • PSMA-targeting ligands
  • radioligands
  • radiopharmaceuticals
  • radiotheranostics
  • nanoparticle-based radiopharmaceuticals
  • targeted radioimaging and radiotherapy
  • nuclear medicine
  • medical oncology

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Published Papers (5 papers)

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Research

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12 pages, 1545 KiB  
Article
Synthesis and Evaluation of 99mTc-Labeled PSMA-Targeted Tracers Based on the Lys-Urea-Aad Pharmacophore for Detecting Prostate Cancer with Single Photon Emission Computed Tomography
by Kelly Lu, Chengcheng Zhang, Zhengxing Zhang, Hsiou-Ting Kuo, Nadine Colpo, François Bénard and Kuo-Shyan Lin
Molecules 2023, 28(13), 5120; https://doi.org/10.3390/molecules28135120 - 29 Jun 2023
Cited by 3 | Viewed by 2518
Abstract
Prostate-specific membrane antigen (PSMA) is a well-validated prostate cancer marker but reported PSMA-targeted tracers derived from the Lys-urea-Glu pharmacophore including the clinically validated [99mTc]Tc-EDDA/HYNIC-iPSMA have high off-target uptake in kidneys, spleen, and salivary glands. In this study, we synthesized and evaluated [...] Read more.
Prostate-specific membrane antigen (PSMA) is a well-validated prostate cancer marker but reported PSMA-targeted tracers derived from the Lys-urea-Glu pharmacophore including the clinically validated [99mTc]Tc-EDDA/HYNIC-iPSMA have high off-target uptake in kidneys, spleen, and salivary glands. In this study, we synthesized and evaluated three novel 99mTc-labeled PSMA-targeted tracers and investigated if the tracers derived from the Lys-urea-Aad pharmacophore could have minimized uptake in off-target organs/tissues. In vitro competition binding assays showed that compared with HYNIC-iPSMA, the three novel ligands had slightly weaker PSMA binding affinity (average Ki = 3.11 vs. 8.96–11.6 nM). Imaging and ex vivo biodistribution studies in LNCaP tumor-bearing mice showed that [99mTc]Tc-EDDA/HYNIC-iPSMA and the three novel tracers successfully visualized LNCaP tumor xenografts in SPECT images and were excreted mainly via the renal pathway. The average tumor uptake at 1 h post-injection varied from 5.40 to 18.8%ID/g, and the tracers derived from the Lys-urea-Aad pharmacophore had much lower uptake in the spleen and salivary glands. Compared with the clinical tracer [99mTc]Tc-EDDA/HYNIC-iPSMA, the Lys-urea-Aad-derived [99mTc]Tc-EDDA-KL01127 had lower background uptake and superior tumor-to-background contrast ratios and is therefore promising for clinical translation to detect prostate cancer lesions with SPECT. Full article
(This article belongs to the Special Issue Targeted Radionuclide Diagnosis and Therapy of Prostate Cancer—From Basic Research to Clinical Perspectives)
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20 pages, 2479 KiB  
Article
[99mTc]Tc-PSMA-T4—Novel SPECT Tracer for Metastatic PCa: From Bench to Clinic
by Michał Maurin, Monika Wyczółkowska, Agnieszka Sawicka, Arkadiusz Eugeniusz Sikora, Urszula Karczmarczyk, Barbara Janota, Marcin Radzik, Dominik Kłudkiewicz, Justyna Pijarowska-Kruszyna, Antoni Jaroń, Wioletta Wojdowska and Piotr Garnuszek
Molecules 2022, 27(21), 7216; https://doi.org/10.3390/molecules27217216 - 25 Oct 2022
Cited by 10 | Viewed by 3183
Abstract
Despite significant advances in nuclear medicine for diagnosing and treating prostate cancer (PCa), research into new ligands with increasingly better biological properties is still ongoing. Prostate-specific membrane antigen (PSMA) ligands show great potential as radioisotope carriers for the diagnosis and therapy of patients [...] Read more.
Despite significant advances in nuclear medicine for diagnosing and treating prostate cancer (PCa), research into new ligands with increasingly better biological properties is still ongoing. Prostate-specific membrane antigen (PSMA) ligands show great potential as radioisotope carriers for the diagnosis and therapy of patients with metastatic PCa. PSMA is expressed in most types of prostate cancer, and its expression is increased in poorly differentiated, metastatic, and hormone-refractory cancers; therefore, it may be a valuable target for the development of radiopharmaceuticals and radioligands, such as urea PSMA inhibitors, for the precise diagnosis, staging, and treatment of prostate cancer. Four developed PSMA-HYNIC inhibitors for technetium-99m labeling and subsequent diagnosis were subjected to preclinical in vitro and in vivo studies to evaluate and compare their diagnostic properties. Among the studied compounds, the PSMA-T4 (Glu-CO-Lys-L-Trp-4-Amc-HYNIC) inhibitor showed the best biological properties for the diagnosis of PCa metastases. [99mTc]Tc-PSMA-T4 also showed effectiveness in single-photon emission computed tomography (SPECT) studies in humans, and soon, its usefulness will be extensively evaluated in phase 2/3 clinical trials. Full article
(This article belongs to the Special Issue Targeted Radionuclide Diagnosis and Therapy of Prostate Cancer—From Basic Research to Clinical Perspectives)
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Review

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16 pages, 2096 KiB  
Review
From Bench to Bedside: Patient-Oriented Radiopharmaceutical Development in Nuclear Medicine Based on the Example of [89Zr]Zr-PSMA-DFO
by Klaus Schomäcker, Felix Dietlein, Sergio Muñoz Vázquez, Feodor Braun, Thomas Fischer, Philipp Krapf, Alexander Drzezga and Markus Dietlein
Molecules 2024, 29(1), 185; https://doi.org/10.3390/molecules29010185 - 28 Dec 2023
Cited by 1 | Viewed by 1708
Abstract
The interdisciplinary possibilities inherent in nuclear medicine offer an opportunity for the patient-centered development of radioactive pharmaceuticals based on specific research questions. This approach provides radiopharmaceutical manufacturers with a robust scientific foundation on which to navigate the regulatory requirements for drug approval laid [...] Read more.
The interdisciplinary possibilities inherent in nuclear medicine offer an opportunity for the patient-centered development of radioactive pharmaceuticals based on specific research questions. This approach provides radiopharmaceutical manufacturers with a robust scientific foundation on which to navigate the regulatory requirements for drug approval laid down by the law. A vivid illustration of this interdisciplinary cooperation has been the development of a Zr-89-labeled PSMA ligand where reliable results have been obtained across various domains, including chemistry, radiochemistry, biochemistry, and preclinical research. This comprehensive process extended to feasibility studies conducted with carefully selected patients from a single nuclear medicine clinic. The approach demonstrates how far close collaboration between different disciplines within nuclear medicine can further the move towards patient-oriented radiopharmaceutical treatments while simultaneously meeting regulatory demands. With such a strategy, innovative radiopharmaceutical solutions can be brought to the market more swiftly and efficiently, in line with the needs of patients. Full article
(This article belongs to the Special Issue Targeted Radionuclide Diagnosis and Therapy of Prostate Cancer—From Basic Research to Clinical Perspectives)
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30 pages, 6500 KiB  
Review
Nanoparticle-Based Radioconjugates for Targeted Imaging and Therapy of Prostate Cancer
by Anna Lankoff, Malwina Czerwińska and Marcin Kruszewski
Molecules 2023, 28(10), 4122; https://doi.org/10.3390/molecules28104122 - 16 May 2023
Cited by 6 | Viewed by 3224
Abstract
Prostate cancer is the second most frequent malignancy in men worldwide and the fifth leading cause of death by cancer. Although most patients initially benefit from therapy, many of them will progress to metastatic castration-resistant prostate cancer, which still remains incurable. The significant [...] Read more.
Prostate cancer is the second most frequent malignancy in men worldwide and the fifth leading cause of death by cancer. Although most patients initially benefit from therapy, many of them will progress to metastatic castration-resistant prostate cancer, which still remains incurable. The significant mortality and morbidity rate associated with the progression of the disease results mainly from a lack of specific and sensitive prostate cancer screening systems, identification of the disease at mature stages, and failure of anticancer therapy. To overcome the limitations of conventional imaging and therapeutic strategies for prostate cancer, various types of nanoparticles have been designed and synthesized to selectively target prostate cancer cells without causing toxic side effects to healthy organs. The purpose of this review is to briefly discuss the selection criteria of suitable nanoparticles, ligands, radionuclides, and radiolabelling strategies for the development of nanoparticle-based radioconjugates for targeted imaging and therapy of prostate cancer and to evaluate progress in the field, focusing attention on their design, specificity, and potential for detection and/or therapy. Full article
(This article belongs to the Special Issue Targeted Radionuclide Diagnosis and Therapy of Prostate Cancer—From Basic Research to Clinical Perspectives)
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39 pages, 7663 KiB  
Review
A Review on the Current State and Future Perspectives of [99mTc]Tc-Housed PSMA-i in Prostate Cancer
by Sara Brunello, Nicola Salvarese, Debora Carpanese, Carolina Gobbi, Laura Melendez-Alafort and Cristina Bolzati
Molecules 2022, 27(9), 2617; https://doi.org/10.3390/molecules27092617 - 19 Apr 2022
Cited by 27 | Viewed by 6512
Abstract
Recently, prostate-specific membrane antigen (PSMA) has gained momentum in tumor nuclear molecular imaging as an excellent target for both the diagnosis and therapy of prostate cancer. Since 2008, after years of preclinical research efforts, a plentitude of radiolabeled compounds mainly based on low [...] Read more.
Recently, prostate-specific membrane antigen (PSMA) has gained momentum in tumor nuclear molecular imaging as an excellent target for both the diagnosis and therapy of prostate cancer. Since 2008, after years of preclinical research efforts, a plentitude of radiolabeled compounds mainly based on low molecular weight PSMA inhibitors (PSMA-i) have been described for imaging and theranostic applications, and some of them have been transferred to the clinic. Most of these compounds include radiometals (e.g., 68Ga, 64Cu, 177Lu) for positron emission tomography (PET) imaging or endoradiotherapy. Nowadays, although the development of new PET tracers has caused a significant drop in single-photon emission tomography (SPECT) research programs and the development of new technetium-99m (99mTc) tracers is rare, this radionuclide remains the best atom for SPECT imaging owing to its ideal physical decay properties, convenient availability, and rich and versatile coordination chemistry. Indeed, 99mTc still plays a relevant role in diagnostic nuclear medicine, as the number of clinical examinations based on 99mTc outscores that of PET agents and 99mTc-PSMA SPECT/CT may be a cost-effective alternative for 68Ga-PSMA PET/CT. This review aims to give an overview of the specific features of the developed [99mTc]Tc-tagged PSMA agents with particular attention to [99mTc]Tc-PSMA-i. The chemical and pharmacological properties of the latter will be compared and discussed, highlighting the pros and cons with respect to [68Ga]Ga-PSMA11. Full article
(This article belongs to the Special Issue Targeted Radionuclide Diagnosis and Therapy of Prostate Cancer—From Basic Research to Clinical Perspectives)
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