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

Kód výsledku v 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>

Výsledek na webu

<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>

Jazyk výsledku

angličtina

Název v původním jazyce

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

Popis výsledku v původním jazyce

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.

Název v anglickém jazyce

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

Popis výsledku anglicky

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.

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

10608 - Biochemistry and molecular biology

Projekt

Výsledek vznikl pri realizaci vícero projektů. Více informací v záložce Projekty.

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Rok uplatnění

2021

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Cancers

ISSN

2072-6694

e-ISSN

—

Svazek periodika

13

Číslo periodika v rámci svazku

8

Stát vydavatele periodika

CH - Švýcarská konfederace

Počet stran výsledku

19

Strana od-do

"nestránkováno"

Kód UT WoS článku

000644007200001

EID výsledku v databázi Scopus

2-s2.0-85104436882