A Novel Method for Real-Time Quantification of Radioligand Binding to Living Tumor Cells In Vitro

• Background: Real-time quantification of radioligand binding to cells under in vivo-like conditions improves evaluation of clinical potential.Materials and Methods: SKOV-3 tumor cells were grown in a monolayer on a thin glass plate placed in a sealable shallow chamber with a continuous flow of 125I-trastuzumab solution. The time-dependent cell binding was measured using a NaI detector, and the binding parameters were derived by computational analysis.Results: The detection efficiency of 125I was 65 cps/kBq for radioligand bound to the cells. Experiments were analyzed to find the values of kon and koff. The resulting kon was 3.2-7.9 x 10(4) M-1 s(-1) and koff was 0.11-4.2 x 10(-5) s(-1).Conclusions: Radioligands can be rapidly evaluated by binding to living cells for selection and optimization of radioconjugates for diagnostic and therapeutic purposes.

Subject headings

MEDICIN OCH HÄLSOVETENSKAP  -- Klinisk medicin -- Cancer och onkologi (hsv//swe)

MEDICAL AND HEALTH SCIENCES  -- Clinical Medicine -- Cancer and Oncology (hsv//eng)

Keyword

binding kinetics

radioligand

flow-through microcuvette

Publication and Content Type

ref (subject category)

art (subject category)