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Gastrin-releasing peptide receptor as a molecular target in experimental anticancer therapy

D B Cornelio1, R Roesler, G Schwartsmann

  • 1Cancer Research Laboratory, Academic Hospital Research Center, Porto Alegre, Brazil.

Annals of Oncology : Official Journal of the European Society for Medical Oncology
|March 14, 2007
PubMed

Insights

Gastrin-releasing peptide receptor (GRPR) is highly expressed in many human cancers, suggesting its potential as a therapeutic target. GRPR antagonists show promise for anticancer treatments and tumor detection.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Gastrin-releasing peptide (GRP) acts as a growth factor in various cancers.
  • Gastrin-releasing peptide receptor (GRPR) antagonists demonstrate antitumoral activity.
  • GRPR is implicated in cancer cell proliferation and survival.

Purpose of the Study:

  • To review the cell surface expression profile of GRPR in human malignancies.
  • To identify potential tumor types for clinical trials involving GRP analogues and antagonists.
  • To evaluate GRPR as a therapeutic target in oncology.

Main Methods:

  • Literature search of Medline, PubMed, and relevant articles from 1971 to 2006.
  • Analysis of published data on GRPR expression in human cancers.
  • Review of experimental evidence for GRPR's role in tumor growth.

Main Results:

  • High expression of GRPR was observed in a wide spectrum of human cancers.
  • GRPR signaling is relevant in various human tumor models.
  • GRPR antagonists exhibit significant in vitro and in vivo antitumoral activity.

Conclusions:

  • GRPR is a promising therapeutic target for human malignancies.
  • GRPR can be utilized for targeted delivery of cytotoxins, immunotoxins, or radioactive compounds.
  • GRPR may serve as a valuable tool for tumor detection and diagnosis.

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