A Novel Method for Real-Time Quantification of Radioligand Binding to Living Tumor Cells In Vitro.
- Resource Type
- Article
- Authors
- Bäck, Tom; Albertsson, Per; Aneheim, Emma; Hultborn, Ragnar; Jacobsson, Lars; Lindegren, Sture; Palm, Stig
- Source
- Cancer Biotherapy & Radiopharmaceuticals. Feb2024, Vol. 39 Issue 1, p75-81. 7p.
- Subject
- *COMPUTER simulation
*IN vitro studies
*OVARIAN tumors
*TRASTUZUMAB
*TIME
*CELL receptors
*RADIOISOTOPES
*DYNAMICS
*DESCRIPTIVE statistics
*RESEARCH funding
*CELL lines
*PHARMACODYNAMICS
- Language
- ISSN
- 1084-9785
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]