Gastrin-releasing peptide receptors (GRPRs), part of the bombesin (BBN) family, are aberrantly overexpressed in many cancers, including those of the breast, prostate, pancreas, and lung, and therefore present an attractive target for cancer diagnosis and therapy. Different bombesin analogs have been radiolabeled and used for imaging diagnosis, staging, evaluation of biochemical recurrence, and assessment of metastatic disease in patients with prostate cancer. Recently, interest has shifted from BBN-like receptor agonists to antagonists, because the latter does not induce adverse effects and demonstrate superior in vivo pharmacokinetics. We review the preclinical and clinical literatures on the use of GRPRs as targets for imaging and therapy of prostate cancer, with a focus on the newer developments and theranostic potential of GRPR peptides.
Molecular imaging and biology. 2018 Aug [Epub]
Lucia Baratto, Hossein Jadvar, Andrei Iagaru
Department of Radiology, Stanford University, Stanford, CA, USA., Department of Radiology, University of Southern California, 2250 Alcazar Street, CSC 102, Los Angeles, CA, 90033, USA. .