The GRPR signaling axis in cancer: Molecular mechanisms and oncogenic outcomes

Júlia Caroline Marcolin1, Martina Lichtenfels2, Rafael Roesler3

  • 1Cancer and Neurobiology Laboratory, Experimental Research Center, Clinical Hospital (CPE-HCPA), Porto Alegre, RS, Brazil; Graduate Program in Biological Sciences: Pharmacology and Therapeutics, Federal University of Rio Grande do Sul, Porto Alegre, RS, Brazil.

Cellular Signalling
|May 12, 2026
PubMed

Insights

Gastrin-releasing peptide receptor (GRPR) signaling is crucial in cancer, regulating tumor progression. Inhibiting GRPR shows therapeutic potential for cancer treatment.

Area of Science:

  • Oncology
  • Molecular Biology
  • Cell Signaling

Background:

  • The gastrin-releasing peptide (GRP) and its receptor (GRPR) signaling axis plays vital roles in physiology.
  • GRPR is increasingly recognized for its significance in cancer biology, being expressed in various tumor types.

Purpose of the Study:

  • To provide a comprehensive review of GRPR-mediated signaling mechanisms in cancer.
  • To integrate evidence from diverse tumor models regarding GRPR's role.
  • To highlight the therapeutic potential of targeting GRPR.

Main Methods:

  • Literature review integrating evidence from multiple tumor models.
  • Analysis of molecular mechanisms of GRPR signaling.
  • Examination of studies on GRPR inhibition and silencing.

Main Results:

  • GRPR activation influences key cancer processes like proliferation, survival, migration, invasion, and angiogenesis.
  • GRPR signaling involves complex intracellular pathways and crosstalk with other signaling systems, including receptor tyrosine kinases.
  • Pharmacological or genetic inhibition of GRPR demonstrates significant antitumor effects.

Conclusions:

  • GRPR acts as a central signaling integrator in tumor progression.
  • GRPR represents a promising therapeutic target for cancer diagnostics, prognostics, and treatments.

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