Publication: Radiometal Complexes as Pharmacokinetic Modifiers: A Potent $^{68}$Ga-Labeled Gastrin-Releasing Peptide Receptor Antagonist Based on the Macrocyclic Metal Chelator NODIA-Me
Radiometal Complexes as Pharmacokinetic Modifiers: A Potent $^{68}$Ga-Labeled Gastrin-Releasing Peptide Receptor Antagonist Based on the Macrocyclic Metal Chelator NODIA-Me
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Schreck, M.-V., Burgard, C., Schmidtke, A., Hierlmeier, I., Stemler, T., Maus, S., Rosar, F., Jung, M., Speicher, A., Ezziddin, S., Holland, J. P., & Bartholomä, M. D. (2023). Radiometal Complexes as Pharmacokinetic Modifiers: A Potent $^{68}$Ga-Labeled Gastrin-Releasing Peptide Receptor Antagonist Based on the Macrocyclic Metal Chelator NODIA-Me. Molecular Pharmaceutics, 20(12), 6463–6473. https://doi.org/10.1021/acs.molpharmaceut.3c00852
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Abstract
The gastrin-releasing peptide receptor (GRPr) is overexpressed in various cancer types including prostate and breast carcinomas, making it an attractive target for molecular imaging and therapy. In this work, we designed a novel GRPr antagonistic probe comprising metal chelator NODIA-Me. This 1,4,7-triazacyclononane-based chelator forms positively charged metal complexes due to its neutral methylimidazole arms. Because a positive charge at the N-terminus of GRPr conjugates is responsible for high receptor affinity as exemplified by th
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- Schreck, Moritz-Valentin
- Burgard, Caroline
- Schmidtke, Alexander
- Hierlmeier, Ina
- Stemler, Tobias
- Maus, Stephan
- Rosar, Florian
- Jung, Martin
- Speicher, Andreas
- Ezziddin, Samer
- Holland, Jason P
- Bartholomä, Mark D
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Schreck, M.-V., Burgard, C., Schmidtke, A., Hierlmeier, I., Stemler, T., Maus, S., Rosar, F., Jung, M., Speicher, A., Ezziddin, S., Holland, J. P., & Bartholomä, M. D. (2023). Radiometal Complexes as Pharmacokinetic Modifiers: A Potent $^{68}$Ga-Labeled Gastrin-Releasing Peptide Receptor Antagonist Based on the Macrocyclic Metal Chelator NODIA-Me. Molecular Pharmaceutics, 20(12), 6463–6473. https://doi.org/10.1021/acs.molpharmaceut.3c00852
