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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
07:41

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators

Published on: February 20, 2018

GRP receptors are present in non small cell lung cancer cells

T W Moody1, F Zia, R Venugopal

  • 1Biomarkers and Prevention Research Branch, National Cancer Institute, Rockville, Maryland 20876, USA.

Journal of Cellular Biochemistry. Supplement
|January 1, 1996
PubMed

Insights

Gastrin-releasing peptide (GRP) receptors in non-small cell lung cancer (NSCLC) cells bind bombesin analogs. These receptors influence cell proliferation and calcium signaling, suggesting a role in NSCLC progression.

Area of Science:

  • Oncology
  • Molecular Biology
  • Cell Biology

Background:

  • Gastrin-releasing peptide (GRP) receptors are known in small cell lung cancer.
  • Their presence and function in non-small cell lung cancer (NSCLC) require further investigation.

Purpose of the Study:

  • To investigate the presence and function of GRP receptors in NSCLC cells.
  • To determine the role of GRP receptors in NSCLC proliferation and signaling pathways.

Main Methods:

  • Radioligand binding assays using (125I-Tyr4) bombesin (BN) or 125I-GRP.
  • Measurement of cytosolic calcium levels and protein kinase C translocation.
  • Assessment of arachidonic acid release and cell proliferation using clonogenic assays.

Main Results:

  • GRP receptors exhibited high-affinity binding to NCI-H720 (lung carcinoid) and NCI-H1299 (large cell carcinoma) NSCLC cells.
  • Bombesin (BN) induced dose-dependent increases in cytosolic calcium and protein kinase C translocation.
  • BN stimulated arachidonic acid release and promoted NCI-H720 cell proliferation, effects reversed by a specific antagonist.

Conclusions:

  • GRP receptors are present in lung carcinoid and NSCLC cells.
  • These receptors mediate signaling pathways involving calcium, protein kinase C, and arachidonic acid release.
  • GRP receptor activation appears to regulate proliferation in NSCLC, suggesting potential therapeutic targets.

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