Towards Targeted Alpha Therapy with Actinium-225: Chelators for Mild Condition Radiolabeling and Targeting PSMA—A Proof of Concept Study

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15110%2F21%3A73606848" target="_blank" >RIV/61989592:15110/21:73606848 - isvavai.cz</a>
Result on the web
<a href="https://www.mdpi.com/2072-6694/13/8/1974" target="_blank" >https://www.mdpi.com/2072-6694/13/8/1974</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.3390/cancers13081974" target="_blank" >10.3390/cancers13081974</a>

Result language
angličtina
Original language name
Towards Targeted Alpha Therapy with Actinium-225: Chelators for Mild Condition Radiolabeling and Targeting PSMA—A Proof of Concept Study
Original language description
In nuclear medicine, therapeutic methods are used increasingly, in which tumors are destroyed by ionizing radiation that cannot or can only be treated insufficiently by other methods like surgery or chemotherapy. Targeted alpha therapy (TAT) is a promising method with increasing importance that facilitates new treatment options for advanced and late-stage cancer diseases. The effectiveness of alpha-emitting radionuclides is characterized by a higher linear energy transfer and a higher biological efficacy, compared to therapeutic approaches with beta emitters. Ac-225 is an alpha emitter with favorable nuclear properties for radiopharmaceutical applications. The aim of our research was to find a universal chelator that enables the attachment of sensitive bio(macro)molecules and allows Ac-225-radiolabeling under mild conditions. An aza-macrocycle-derived mcp chelator with functional groups for universal connection of biomolecules using convenient click chemistry was developed for the Ac-225-labeling. The resulting Ac-225-radioconjugates were analyzed in vitro and in vivo, showing a high receptor affinity on tumor cells and a high tumor accumulation in tumor-bearing mice.
Czech name
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Czech description
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Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10608 - Biochemistry and molecular biology

Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Publication year
2021
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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