1. Theranostic Prospects of Gastrin-Releasing Peptide Receptor–Radioantagonists in Oncology
- Author
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Theodosia Maina, Harshad R. Kulkarni, Berthold A. Nock, Aviral Singh, and Richard P. Baum
- Subjects
Oncology ,medicine.medical_specialty ,medicine.drug_class ,Theranostic Nanomedicine ,030218 nuclear medicine & medical imaging ,03 medical and health sciences ,Prostate cancer ,chemistry.chemical_compound ,0302 clinical medicine ,In vivo ,Neoplasms ,Internal medicine ,medicine ,Gastrin-releasing peptide receptor ,Animals ,Humans ,Radiology, Nuclear Medicine and imaging ,Receptor ,Radiation ,business.industry ,Cancer ,Bombesin ,General Medicine ,medicine.disease ,Receptor antagonist ,Receptors, Bombesin ,chemistry ,Positron-Emission Tomography ,030220 oncology & carcinogenesis ,Radionuclide therapy ,Tomography, X-Ray Computed ,business - Abstract
Gastrin-releasing peptide receptors (GRPRs) represent attractive targets for cancer diagnosis and therapy owing to their overexpression in widespread human tumors. Bombesin (BBN) analogues coupled to suitable chelators for stable radiometal binding have been proposed for diagnostic imaging and radionuclide therapy (theranostics) of GRPR-positive tumors. Recently, interest has shifted from BBN-like receptor agonists to GRPR-radioantagonists, because radioantagonists do not induce adverse effects after injection to patients and display superior pharmacokinetic in vivo profiles. Thus, they seem more advantageous for clinical use compared to agonists. Newer developments highlighting the theranostic potential of GRPR-radioantagonists in cancer patient management are presented herein.
- Published
- 2017