Der Einsatz von Steroidhormonen als Trägermoleküle zur Anreicherung von Radionukliden in Tumorzellen erscheint als eine interessante neue Therapiestrategie vor dem Hintergrund, daß zahlreiche Karzinome des weiblichen Genitaltrakts und der Mamma Hormonrezeptoren exprimieren, und daß Radionuklide, die Strahlen mit extrem kurzer Reichweite emittieren (Auger-Elektronen), letale Dosen ionisierender Strahlen innerhalb einzelner Zellen deponieren, theoretisch ohne Beeinträchtigung von Nachbarzellen. In Kulturen von humanen MCF-7 MammakarzinomzeUen wiesen wir die Zytotoxizität des Au-ger-Elektronen-emittierenden Radiosteroids 16alpha-[125I]Jod-17be-ta-Östradiol für wachsende Zellen nach und belegten, daß dieser Effekt durch Östrogenrezeptoren vermittelt wird. Die maximale rezeptorvermittelte Letalität wurde bei Radioaktivität erreicht, die bei fehlender Vermittlung durch Rezeptoren nur minimale Toxizität zeigten.

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