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The overexpression of gastrin-releasing peptide receptors (GRPRs) in prostate and breast cancer provides opportunities for diagnosis and therapy with GRPR-directed radiopeptides.
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Radiolabeled analogues of amphibian bombesin have been developed for GRPR-targeted tumor diagnosis and therapy.
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GRPR-radioantagonists, although unable to internalize in cancer cells, show considerable advantages for tumor targeting in human over their agonist counterparts, such as higher biosafety and superior
Theranostic Prospects of Gastrin-Releasing Peptide Receptor–Radioantagonists in Oncology
Section snippets
Key points
Toward gastrin-releasing peptide receptor antagonists and their radiolabeled analogues for use in gastrin-releasing peptide receptor–expressing tumor imaging and therapy
The BBN-like peptide agonists after systemic administration exert a wide spectrum of biological actions on binding and activation of the GRPR, such as the release of gastrointestinal peptide hormones, the stimulation of exocrine gland secretion, and the contraction of smooth musculature, all synergistically translating into potent adverse reactions in the gastrointestinal system.43, 45, 46, 47, 49, 50 Furthermore, they have been implicated in the pathogenesis of human cancers via autocrine
Theranostic prospects of gastrin-releasing peptide receptor radioantagonists in oncology: concluding remarks
Theranostic approaches for GRPR-expressing human tumors, such as the frequently occurring prostate and breast cancer, are expected to enter the clinic in the near future as a result of the continuous emergence of state-of-the-art GRPR radioantagonists.74, 97, 107, 109 As shown in this brief survey, GRPR radioantagonists are associated to higher biosafety and potent targeting of tumor lesions combined with attractive pharmacokinetics in animal models and patients compared with agonists. These
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Cited by (44)
Gastrin-releasing peptide receptor as a theranostic target in breast cancer: a systematic scoping review
2024, Seminars in Nuclear Medicinep-NCS-Bn-NODAGA as a bifunctional chelator for radiolabeling with the <sup>186</sup>Re/<sup>99m</sup>Tc-tricarbonyl core: Radiochemistry with model complexes and a GRPR-targeting peptide
2022, Nuclear Medicine and BiologyCitation Excerpt :The first generation of targeting vectors for GRPR was comprised of agonists (vectors designed to be internalized into the cell). These agonists were successfully utilized in targeting of GRPR in prostate cancer models [9–11]; however, they were also associated with adverse gastrointestinal reactions in patients [12]. Recently, it has been shown that antagonistic vectors (little to no cell internalization) outperform their agonist counterparts in vivo in terms of tumor uptake.
Peptide radiopharmaceuticals for targeted diagnosis & therapy of human tumors
2022, Nuclear Medicine and Molecular Imaging: Volume 1-4SPECT Radiochemistry
2021, Molecular Imaging: Principles and PracticeNovel Agents and Future Perspectives on Theranostics
2021, Seminars in Radiation OncologyCitation Excerpt :Gastrin-releasing peptide receptors are highly expressed in several solid tumors including prostate, breast and small cell lung cancer.34 Radioantagonists of the gastrin-releasing peptide receptors are emerging theranostic treatment modalities in solid cancers.35 Phase I/IIa clinical trials are underway to determine the safety, tolerability, dosimetry and anti-tumor activity of 177LuNeoB in patients with GRPR positive solid tumors (NCT03872778).
Disclosure: Drs T. Maina and B.A. Nock participate in an AAA-contract on NeoBOMB1 and are coinventors in a patent owned by AAA. Drs H. Kulkarni, A. Singh, and R. Baum have nothing to disclose.