Elsevier

PET Clinics

Volume 12, Issue 3, July 2017, Pages 297-309
PET Clinics

Theranostic Prospects of Gastrin-Releasing Peptide Receptor–Radioantagonists in Oncology

https://doi.org/10.1016/j.cpet.2017.02.007Get rights and content

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Key points

  • The overexpression of gastrin-releasing peptide receptors (GRPRs) in prostate and breast cancer provides opportunities for diagnosis and therapy with GRPR-directed radiopeptides.

  • Radiolabeled analogues of amphibian bombesin have been developed for GRPR-targeted tumor diagnosis and therapy.

  • 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

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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    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.

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