Neuropeptide G Protein-Coupled Receptors as Oncotargets

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Updated: Feb 7, 2026

Quantifying Agonist Activity at G Protein-coupled Receptors
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Quantifying Agonist Activity at G Protein-coupled Receptors

Published on: December 26, 2011

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Terry W Moody1, Irene Ramos-Alvarez2, Robert T Jensen2

  • 1Department of Health and Human Services, National Cancer Institute, Center for Cancer Research, National Institute of Diabetes, Digestive, and Kidney Disease (NIDDK), Bethesda, MD, United States.

Frontiers in Endocrinology
|July 17, 2018
PubMed

Insights

Neuropeptide receptors like bombesin and neurotensin promote cancer growth, while somatostatin inhibits it. Targeting these receptors offers new avenues for cancer detection and treatment.

Area of Science:

  • Oncology
  • Molecular Endocrinology
  • G protein-coupled receptor (GPCR) signaling

Background:

  • Neuropeptide G protein-coupled receptors (GPCRs) are frequently overexpressed in various cancer types.
  • In small cell lung cancer (SCLC), bombesin (BB) and neurotensin (NTS) peptides act as autocrine growth factors, stimulating tumor cell proliferation.
  • Vasoactive intestinal peptide (VIP) can enhance BB-like peptide and NTS secretion, further promoting SCLC growth.

Purpose of the Study:

  • To review the role of neuropeptide receptors in cancer.
  • To explore how bombesin (BB), neurotensin (NTS), vasoactive intestinal peptide (VIP), and somatostatin (SST) receptors can be leveraged for cancer diagnosis and therapy.
  • To highlight the therapeutic potential of targeting these receptor pathways.

Main Methods:

  • Literature review focusing on neuropeptide receptor function in cancer.
  • Analysis of studies investigating BB, NTS, VIP, and SST receptor roles in tumor growth and proliferation.
  • Examination of therapeutic strategies involving receptor antagonists, drug conjugates, and receptor analogs.

Main Results:

  • BB and NTS receptor activation stimulates cancer cell growth, with BB-drug conjugates and antagonists showing inhibitory effects.
  • Somatostatin (SST) inhibits autocrine growth factor secretion in neuroendocrine tumors (NETs), reducing proliferation.
  • SST analogs, like radiolabeled octreotide, are valuable for tumor localization, diagnosis, and treatment of NETs.

Conclusions:

  • Neuropeptide receptors represent promising targets for novel cancer therapies.
  • Targeting BB, NTS, VIP, and SST receptors offers potential for early cancer detection and effective treatment strategies.
  • The dual role of these receptors in promoting or inhibiting cancer highlights their significance in oncology.
Keywords:
bombesincancer GPCRcancer RTKcancer signal transductionneurotensinpituitary adenylate cyclase activating polypeptide (PACAP)somatostatinvasoactive intestinal peptide

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