The DOI matches its Crossref record; 266 of the 283 references it cites were found in a registry or an index.
Development of targeted alpha particle therapy for solid tumors.
Open accessAbstract
Targeted alpha-particle therapy (TAT) aims to selectively deliver radionuclides emitting α-particles (cytotoxic payload) to tumors by chelation to monoclonal antibodies, peptides or small molecules that recognize tumor-associated antigens or cell-surface receptors. Because of the high linear energy transfer (LET) and short range of alpha (α) particles in tissue, cancer cells can be significantly damaged while causing minimal toxicity to surrounding healthy cells. Recent clinical studies have demonstrated the remarkable efficacy of TAT in the treatment of metastatic, castration-resistant prostate cancer. In this comprehensive review, we discuss the current consensus regarding the properties of the α-particle-emitting radionuclides that are potentially relevant for use in the clinic; the TAT-mediated mechanisms responsible for cell death; the different classes of targeting moieties and radiometal chelators available for TAT development; current approaches to calculating radiation dosimetry for TATs; and lead optimization via medicinal chemistry to improve the TAT radiopharmaceutical properties. We have also summarized the use of TATs in pre-clinical and clinical studies to date.
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“Moreover, the isomeric γ emissions with energy suitable for SPECT imaging grants 225Ac the theranostic possibility (68, 69).”
From Alpha-peptide receptor radionuclide therapy using actinium-225 labeled somatostatin receptor agonists and antagonists (2022) · cites this paper as [69]
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17 of the 283 references couldn’t be matched to a known paper.
Research works printed but not linked: 6
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Antibody–drug conjugates come of age in oncology
Dumontet, C., Reichert, J. M., Senter, P. D., Lambert, J. M., & Beck, A. (2023) · Nature Reviews Drug Discovery · doi:10.1038/s41573-023-00709-2 · Cited by 903
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Eychenne, R., Bouvry, C., Bourgeois, M., Loyer, P., Benoist, É., & Lepareur, N. (2020) · Molecules · doi:10.3390/molecules25174012 · Cited by 133
Hooijman, E. L., Radchenko, V., Ling, S. W., Konijnenberg, M., Brabander, T., Koolen, S. L. W., & de Blois, E. (2024) · EJNMMI Radiopharmacy and Chemistry · doi:10.1186/s41181-024-00239-1 · Cited by 91
Metadata
- Authors
- Tafreshi, N. K., Doligalski, M. L., Tichacek, C. J., Pandya, D. N., Budzevich, M. M., El-Haddad, G., Khushalani, N. I., Moros, E. G., McLaughlin, M. L., Wadas, T. J., & Morse, D. L.
- Affiliations
- Moffitt Cancer Center (US)
- Wake Forest University Health Sciences (US)
- University of South Florida (US)
- West Virginia University (US)
- Corresponding author
- Morse, David L.
- ORCID
- Venue
- Molecules
- Publisher
- MDPI AG
- Published
- 2019-11-26
- Volume
- 24
- Issue
- 23
- Pages
- 4314
- ISSN
- 1420-3049 (ISSN-L)
- PMC
- PMC6930656
- OpenAlex
- W2990493095
- Cited by
- 157
- References
- 283
- Citations by year
- 2026: 21 · 2025: 25 · 2024: 24 · 2023: 26 · 2022: 23 · 2021: 30 · 2020: 7
- FWCI
- 2.25
- Type
- journal article
- Language
- en
- Open access
- gold
- dx.doi.org
- Licence
- Locations
- Molecules (publishedVersion, cc-by)
- PubMed Central (publishedVersion, cc-by)
- PubMed (publishedVersion)
- The Research Repository @ WVU (West Virginia University) (submittedVersion, cc-by)
- Funders
- Melanoma Research Alliance
- National Institutes of Health
- National Cancer Institute (P50CA168536)
- Topics
- Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Radiopharmaceutical Chemistry and Applications
- Physical Sciences › Physics and Astronomy › Radiation › Radioactivity and Radon Measurements
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Chemical Reactions and Isotopes
- Keywords
- alpha-emitting radionuclides, radiopharmaceuticals, linear energy transfer, tumor targeting, radiation dosimetry, castration-resistant prostate cancer, metastatic prostate cancer, cell death mechanisms, solid tumors
- MeSH terms
- Alpha Particles, Animals, Antibodies, Monoclonal, Humans, Neoplasms, Radioisotopes, Radiometry, Radiopharmaceuticals
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