Unexpected Sensitivity of sst2 Antagonists to N-Terminal Radiometal Modifications
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Chelated somatostatin agonists have been shown to be sensitive to N-terminal radiometal modifications, with Ga-DOTA agonists having significantly higher binding affinity than their Lu-, In-, and Y-DOTA correlates. Recently, somatostatin antagonists have been successfully developed as alternative tracers to agonists. The aim of this study was to evaluate whether chelated somatostatin antagonists are also sensitive to radiometal modifications and how. We have synthesized 3 different somatostatin antagonists, DOTA-p-NO(2)-Phe-c[D-Cys-Tyr-D-Aph(Cbm)-Lys-Thr-Cys]-D-Tyr-NH(2), DOTA-Cpa-c[D-Cys-Aph(Hor)-D-Aph(Cbm)-Lys-Thr-Cys]-D-Tyr-NH(2) (DOTA-JR11), and DOTA-p-Cl-Phe-c[D-Cys-Tyr-D-Aph(Cbm)-Lys-Thr-Cys]-D-Tyr-NH(2), and added various radiometals including In(III), Y(III), Lu(III), Cu(II), and Ga(III). We also replaced DOTA with 1,4,7-triazacyclononane,1-glutaric acid-4,7-acetic acid (NODAGA) and added Ga(III). The binding affinity of somatostatin receptors 1 through 5 was evaluated in all cases. In all 3 resulting antagonists, the Ga-DOTA analogs were the lowest-affinity radioligands, with a somatostatin receptor 2 binding affinity up to 60 times lower than the respective Y-DOTA, Lu-DOTA, or In-DOTA compounds. Interestingly, however, substitution of DOTA by the NODAGA chelator was able to increase massively its binding affinity in contrast to the Ga-DOTA analog. The 3 NODAGA analogs are antagonists in functional tests. In vivo biodistribution studies comparing (68)Ga-DOTATATE agonist with (68)Ga-DOTA-JR11 and (68)Ga-NODAGA-JR11 showed not only that the JR11 antagonist radioligands were superior to the agonist ligands but also that (68)Ga-NODAGA-JR11 was the tracer of choice and preferable to (68)Ga-DOTA-JR11 in transplantable HEK293-hsst(2) tumors in mice. One may therefore generalize that somatostatin receptor 2 antagonists are sensitive to radiometal modifications and may preferably be coupled with a (68)Ga-NODAGA chelator-radiometal complex.
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68Ga-DOTA-JR11 and -LM3, which have drastically lower affinities for SSTR2 (approximately 150-fold and 60-fold, respectively) than 68Ga-DOTATATE, showed higher tumor uptake.
“Interestingly, 68Ga-DOTA-JR11 and -LM3, which have drastically lower affinities for SSTR2 (approximately 150-fold and 60-fold, respectively) than 68Ga-DOTATATE, showed higher tumor uptake (132).”
From Alpha-peptide receptor radionuclide therapy using actinium-225 labeled somatostatin receptor agonists and antagonists (2022) · cites this paper as [132]
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- Authors
- Fani, M., Braun, F., Waser, B., Beetschen, K., Cescato, R., Erchegyi, J., Rivier, J. E., Weber, W. A., Maecke, H. R., & Reubi, J. C.
- Affiliations
- University Medical Center Freiburg (DE)
- University of Bern (CH)
- Salk Institute for Biological Studies (US)
- Venue
- Journal of Nuclear Medicine
- Publisher
- Society of Nuclear Medicine
- Published
- 2012-07-31
- Volume
- 53
- Issue
- 9
- Pages
- 1481-1489
- ISSN
- 0161-5505 (ISSN-L)
- 2159-662X
- OpenAlex
- W2018848884
- Cited by
- 172
- References
- 28
- Citations by year
- 2026: 10 · 2025: 18 · 2024: 15 · 2023: 15 · 2022: 18 · 2021: 18 · 2020: 17 · 2019: 10 · 2018: 12 · 2017: 16 · 2016: 7 · 2015: 7 · 2014: 8 · 2013: 1
- FWCI
- 3.86
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- Journal of Nuclear Medicine (publishedVersion)
- PubMed (publishedVersion)
- Bern Open Repository and Information System (University of Bern) (submittedVersion)
- Topics
- Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Radiopharmaceutical Chemistry and Applications
- Health Sciences › Medicine › Epidemiology › Neuroendocrine Tumor Research Advances
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuropeptides and Animal Physiology
- Keywords
- somatostatin receptor 2, DOTA chelator, NODAGA, gallium-68, indium-111, lutetium-177, copper-64, binding affinity, tissue distribution, tumor imaging, somatostatin receptor imaging
- MeSH terms
- Animals, Female, Gallium Radioisotopes, Heterocyclic Compounds, 1-Ring, Humans, Somatostatin, Gene Expression Regulation, Neoplastic, Receptors, Somatostatin, Mice, HEK293 Cells, Hydrophobic and Hydrophilic Interactions
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