Abstract
Methods
Boroaryl functionalised biotin was prepared with a PEG linker and radiolabelled by incubation with 18F in acidified aqueous solution. Cells expressing high (SKBr3), medium (MDA-MB-453) and low (MDA-MB-468) levels of HER-2 were pre-incubated with Neutravidin™-conjugated trastuzumab, washed, and then incubated with 18F-PEG-biotin.
Results
The 18F-fluorination of boroaryl-PEG-biotin was much more efficient than reported for other versions of boroaryl-biotin. The novel 18F-PEG-biotin was demonstrated to bind to HER-2-expressing cells in-vitro pre-incubated with Neutravidin™-conjugated trastuzumab.
Conclusion
Biotin can be functionalised with boroaryl and readily 18F-radiolabelled in aqueous solution and will bind to cells pre-incubated with Neutravidin™–antibody conjugates.
Highlights
¿ Boroaryl-biotin precursor is prepared. ¿ Rapid 18F-fluorination is demonstrated. ¿ HER-2 expressing breast cancer cells pre-treated with trastuzumab–Neutravidin™. ¿ 18F-PEG-biotin binding to pre-treated cells corresponds with HER-2 expression.
| Original language | English |
|---|---|
| Pages (from-to) | 1395-1400 |
| Number of pages | 6 |
| Journal | Applied Radiation and Isotopes |
| Volume | 69 |
| Issue number | 10 |
| Early online date | 11 May 2011 |
| DOIs | |
| Publication status | Published - Oct 2011 |
Fingerprint
Keywords
- 18F
- PET
- Neutravidin™
- breast cancer cells
- Biotin
Cite this
18F-PEG-biotin : Precursor (boroaryl-PEG-biotin) synthesis, 18F-labelling and an in-vitro assessment of its binding to NeutravidinTM -trastuzumab pre-treated cells. / Smith, Timothy Andrew Davies; Simpson, Michael; Cheyne, Richard William; Trembleau, Laurent Alain Claude.
In: Applied Radiation and Isotopes, Vol. 69, No. 10, 10.2011, p. 1395-1400.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - 18F-PEG-biotin
T2 - Precursor (boroaryl-PEG-biotin) synthesis, 18F-labelling and an in-vitro assessment of its binding to NeutravidinTM -trastuzumab pre-treated cells
AU - Smith, Timothy Andrew Davies
AU - Simpson, Michael
AU - Cheyne, Richard William
AU - Trembleau, Laurent Alain Claude
PY - 2011/10
Y1 - 2011/10
N2 - In terms of nuclear decay 18F is the most ideal PET nuclide but its short t1/2 precludes its use for directly labelling whole antibodies due to their long blood residence times. Pre-targeted imaging using affinity systems such as Neutravidin™–biotin facilitates the application of short-lived nuclides by their attachment to biotin for imaging cell surface proteins targeted with Neutravidin™-conjugated antibodies. Methods Boroaryl functionalised biotin was prepared with a PEG linker and radiolabelled by incubation with 18F in acidified aqueous solution. Cells expressing high (SKBr3), medium (MDA-MB-453) and low (MDA-MB-468) levels of HER-2 were pre-incubated with Neutravidin™-conjugated trastuzumab, washed, and then incubated with 18F-PEG-biotin. Results The 18F-fluorination of boroaryl-PEG-biotin was much more efficient than reported for other versions of boroaryl-biotin. The novel 18F-PEG-biotin was demonstrated to bind to HER-2-expressing cells in-vitro pre-incubated with Neutravidin™-conjugated trastuzumab. Conclusion Biotin can be functionalised with boroaryl and readily 18F-radiolabelled in aqueous solution and will bind to cells pre-incubated with Neutravidin™–antibody conjugates. Highlights ¿ Boroaryl-biotin precursor is prepared. ¿ Rapid 18F-fluorination is demonstrated. ¿ HER-2 expressing breast cancer cells pre-treated with trastuzumab–Neutravidin™. ¿ 18F-PEG-biotin binding to pre-treated cells corresponds with HER-2 expression.
AB - In terms of nuclear decay 18F is the most ideal PET nuclide but its short t1/2 precludes its use for directly labelling whole antibodies due to their long blood residence times. Pre-targeted imaging using affinity systems such as Neutravidin™–biotin facilitates the application of short-lived nuclides by their attachment to biotin for imaging cell surface proteins targeted with Neutravidin™-conjugated antibodies. Methods Boroaryl functionalised biotin was prepared with a PEG linker and radiolabelled by incubation with 18F in acidified aqueous solution. Cells expressing high (SKBr3), medium (MDA-MB-453) and low (MDA-MB-468) levels of HER-2 were pre-incubated with Neutravidin™-conjugated trastuzumab, washed, and then incubated with 18F-PEG-biotin. Results The 18F-fluorination of boroaryl-PEG-biotin was much more efficient than reported for other versions of boroaryl-biotin. The novel 18F-PEG-biotin was demonstrated to bind to HER-2-expressing cells in-vitro pre-incubated with Neutravidin™-conjugated trastuzumab. Conclusion Biotin can be functionalised with boroaryl and readily 18F-radiolabelled in aqueous solution and will bind to cells pre-incubated with Neutravidin™–antibody conjugates. Highlights ¿ Boroaryl-biotin precursor is prepared. ¿ Rapid 18F-fluorination is demonstrated. ¿ HER-2 expressing breast cancer cells pre-treated with trastuzumab–Neutravidin™. ¿ 18F-PEG-biotin binding to pre-treated cells corresponds with HER-2 expression.
KW - 18F
KW - PET
KW - Neutravidin™
KW - breast cancer cells
KW - Biotin
U2 - 10.1016/j.apradiso.2011.05.005
DO - 10.1016/j.apradiso.2011.05.005
M3 - Article
VL - 69
SP - 1395
EP - 1400
JO - Applied Radiation and Isotopes
JF - Applied Radiation and Isotopes
SN - 0969-8043
IS - 10
ER -