Targeting GRPR in urological cancers—from basic research to clinical application
- Resource Type
- Authors
- Rosalba Mansi; Jean Claude Reubi; Helmut R. Mäcke; Achim Fleischmann
- Source
- Nature Reviews Urology. 10:235-244
- Subject
- Regulation of gene expression
Urologic Neoplasms
Pathology
medicine.medical_specialty
Biomedical Research
business.industry
Urology
medicine.medical_treatment
Urological cancers
Gene Expression Regulation, Neoplastic
Receptors, Bombesin
Radiation therapy
Drug Delivery Systems
medicine.anatomical_structure
Prostate
Basic research
Gastrin-releasing peptide
medicine
Cancer research
Animals
Humans
Cytotoxic T cell
Receptor
business
hormones, hormone substitutes, and hormone antagonists
- Language
- ISSN
- 1759-4820
1759-4812
Gastrin releasing peptide (GRP) is a regulatory peptide that acts through its receptor (GRPR) to regulate physiological functions in various organs. GRPR is overexpressed in neoplastic cells of most prostate cancers and some renal cell cancers and in the tumoral vessels of urinary tract cancers. Thus, targeting these tumours with specifically designed GRP analogues has potential clinical application. Potent and specific radioactive, cytotoxic or nonradioactive GRP analogues have been designed and tested in various animal tumour models with the aim of receptor targeting for tumour diagnosis or therapy. All three categories of compound were found suitable for tumour targeting in animal models. The cytotoxic and nonradioactive GRP analogues have not yet shown convincing tumour-reducing effects in human trials; however, the first clinical studies of radioactive GRP analogues--both agonists and antagonists--suggest promising opportunities for both diagnostic tumour imaging and radiotherapy of prostate and other GRPR-expressing cancers.