1. A Novel Method for Real-Time Quantification of Radioligand Binding to Living Tumor Cells In Vitro.
- Author
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Bäck, Tom, Albertsson, Per, Aneheim, Emma, Hultborn, Ragnar, Jacobsson, Lars, Lindegren, Sture, and Palm, Stig
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COMPUTER simulation , *IN vitro studies , *OVARIAN tumors , *TRASTUZUMAB , *TIME , *CELL receptors , *RADIOISOTOPES , *DYNAMICS , *DESCRIPTIVE statistics , *RESEARCH funding , *CELL lines , *PHARMACODYNAMICS - Abstract
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 × 104 M−1 s−1 and koff was 0.11–4.2 × 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. [ABSTRACT FROM AUTHOR]
- Published
- 2024
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