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Published on: January 7, 2019
Design and evaluation of novel radiolabelled VIP derivatives for tumour targeting
Christine Rangger1, Anna Helbok, Meltem Ocak
1Clinical Department of Nuclear Medicine, Innsbruck Medical University, Innsbruck, Austria.
Background:
Vasoactive intestinal peptide (VIP) receptors are overexpressed in a broad variety of tumours. For the detection of these tumours, novel chemically modified and shortened VIP derivatives were designed.
Materials And Methods:
1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA)-derivatised VIP analogues were radiolabelled with (111)In and in vitro and in vivo behaviour was evaluated using stability and internalisation assays, as well as an initial biodistribution study.
Results:
Radiolabelling of the VIP analogues resulted in high radiochemical yields, without need for further purification steps. Stability of the VIP derivatives was variable and cell uptake studies in VIP receptor-positive cell lines revealed that only a limited number of derivatives were internalised. In the tumour mouse model, no specific tumour targeting was shown.
Conclusion:
Since the tested VIP derivatives exhibited impaired in vitro and in vivo characteristics alternative modifications to increase their stability while retaining receptor affinity should be considered to enable the use of synthetic VIP analogues for tumour targeting.
Insights
Novel vasoactive intestinal peptide (VIP) derivatives showed poor tumor targeting. Further modifications are needed to improve stability and receptor affinity for effective cancer detection using VIP analogues.
Area of Science:
- Biochemistry
- Radiochemistry
- Oncology
Background:
- Vasoactive intestinal peptide (VIP) receptors are frequently overexpressed in various tumor types.
- This overexpression presents a potential target for diagnostic and therapeutic strategies.
Purpose of the Study:
- To design and evaluate novel, chemically modified, and shortened VIP derivatives for tumor detection.
- To assess the in vitro and in vivo behavior of these derivatives.
Main Methods:
- VIP analogues were derivatized with 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA).
- Derivatives were radiolabeled with Indium-111 ((111)In).
- In vitro (stability, internalization) and in vivo (biodistribution in a mouse model) studies were performed.
Main Results:
- High radiochemical yields were achieved during radiolabeling.
- The stability of the VIP derivatives varied.
- Limited internalization was observed in VIP receptor-positive cell lines.
- No specific tumor targeting was demonstrated in a mouse tumor model.
Conclusions:
- The tested VIP derivatives displayed suboptimal in vitro and in vivo characteristics.
- Alternative modifications are necessary to enhance stability while maintaining VIP receptor affinity.
- Further development is required for the successful application of synthetic VIP analogues in tumor targeting.
