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Special Issue "Targeted Radionuclide Diagnosis and Therapy of Prostate Cancer—From Basic Research to Clinical Perspectives"

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

Deadline for manuscript submissions: 31 October 2023 | Viewed by 3812

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Special Issue Editor

Prof. Dr. Anna Lankoff

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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 2300 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

Published Papers (3 papers)

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Research

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Open AccessArticle

[^99mTc]Tc-PSMA-T4—Novel SPECT Tracer for Metastatic PCa: From Bench to Clinic

Michał Maurin

Monika Wyczółkowska

Agnieszka Sawicka

Arkadiusz Eugeniusz Sikora

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 1 | Viewed by 759

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 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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Open AccessReview

Nanoparticle-Based Radioconjugates for Targeted Imaging and Therapy of Prostate Cancer

Anna Lankoff

Malwina Czerwińska

and

Marcin Kruszewski

Molecules 2023, 28(10), 4122; https://doi.org/10.3390/molecules28104122 - 16 May 2023

Viewed by 408

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 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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Open AccessReview

A Review on the Current State and Future Perspectives of [^99mTc]Tc-Housed PSMA-i in Prostate Cancer

Laura Melendez-Alafort

and

Cristina Bolzati

Molecules 2022, 27(9), 2617; https://doi.org/10.3390/molecules27092617 - 19 Apr 2022

Cited by 8 | Viewed by 2241

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 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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