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G protein-coupled receptors as novel therapeutic targets in non-small-cell lung cancer

Lijuan Ma1,2, Pengju Zhang1, Jin-Peng Sun1,3,4

  • 1Department of Biochemistry and Molecular Biology, Key Laboratory Experimental Teratology of the Ministry of Education, School of Basic Medical Sciences, Cheeloo College of Medicine, Shandong University, Jinan, Shandong, China.

Medical Review (2021)
|January 1, 2026
PubMed

Insights

G protein-coupled receptors (GPCRs) are key drivers in non-small-cell lung cancer (NSCLC) development and progression. Targeting GPCRs offers therapeutic potential but faces significant challenges in NSCLC treatment.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • G protein-coupled receptors (GPCRs) regulate vital cellular functions including proliferation, differentiation, and communication.
  • GPCRs are implicated in the initiation and progression of various cancers, including non-small-cell lung cancer (NSCLC).

Purpose of the Study:

  • To review the multifaceted roles of GPCRs, including understudied ones, in non-small-cell lung cancer (NSCLC) oncogenesis and progression.
  • To summarize current knowledge on GPCR functions in NSCLC, focusing on tumor development, progression, and therapy resistance.
  • To evaluate the therapeutic potential of targeting GPCR-driven signaling pathways in NSCLC.

Main Methods:

  • Literature review focusing on GPCRs in non-small-cell lung cancer.
  • Analysis of GPCR involvement in tumor development, progression, and drug resistance.
  • Evaluation of current and emerging therapeutic strategies targeting GPCRs in NSCLC.

Main Results:

  • GPCRs significantly contribute to NSCLC oncogenesis, tumor growth, metastasis, and resistance to therapies.
  • Several GPCRs, including those previously understudied, play critical roles in NSCLC progression.
  • Targeting GPCRs presents a promising avenue for novel NSCLC therapies, though challenges remain.

Conclusions:

  • GPCRs are crucial regulators in NSCLC, offering potential therapeutic targets.
  • Understanding GPCR signaling in NSCLC is essential for developing effective anticancer treatments.
  • Addressing knowledge gaps and overcoming challenges in GPCR-targeted therapy is vital for improving NSCLC patient outcomes.
Keywords:
G protein-coupled receptorbiomarkersnon-small-cell lung canceroncogenetumor suppressor

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