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Updated: Feb 12, 2026

Building Up a High-throughput Screening Platform to Assess the Heterogeneity of HER2 Gene Amplification in Breast Cancers
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Building Up a High-throughput Screening Platform to Assess the Heterogeneity of HER2 Gene Amplification in Breast Cancers

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GPCRs profiling and identification of GPR110 as a potential new target in HER2+ breast cancer

Raksha R Bhat1, Puja Yadav1, Debashish Sahay1

  • 1Department of Pharmacy Practice and Translational Research, University of Houston, 4849 Calhoun St, Houston, TX, 77204, USA.

Breast Cancer Research and Treatment
|March 26, 2018
PubMed
Abstract

Insights

G protein-coupled receptors (GPCRs) are implicated in HER2+ breast cancer (BC). GPR110 is overexpressed in resistant cells and promotes tumor growth and spread, suggesting it as a potential therapeutic target.

Area of Science:

  • Oncology
  • Molecular Biology
  • Genomics

Background:

  • G protein-coupled receptors (GPCRs) are a major class of drug targets, but their roles in HER2-positive breast cancer (BC) are largely unexplored.
  • Understanding GPCR expression and function is crucial for developing novel therapies against HER2+ BC, especially in drug-resistant contexts.

Purpose of the Study:

  • To investigate the gene expression profiles of GPCRs in tumorigenic and anti-HER2 drug-resistant HER2+ BC cells.
  • To identify specific GPCRs that may play a role in the progression and therapeutic resistance of HER2+ BC.

Main Methods:

  • Profiled 352 GPCRs in tumorigenic (Aldefluor+) versus non-tumorigenic (Aldefluor-) and anti-HER2 resistant versus parental HER2+ BT474 cells.
  • Validated GPCR candidates in multiple HER2+ BC cell lines and patient datasets.
  • Assessed the functional impact of GPR110 knockdown on cell growth, mammosphere formation, and invasion in parental and resistant cells.

Main Results:

  • Adhesion and Class A GPCRs were upregulated in tumorigenic and resistant populations, respectively.
  • GPR110 was consistently overexpressed across multiple HER2+ BC models and patient tumors, particularly in resistant and tumorigenic cells.
  • GPR110 knockdown significantly inhibited cell growth, migration, invasion, and mammosphere formation in both parental and resistant HER2+ BC cells.

Conclusions:

  • GPR110 is a key GPCR overexpressed in HER2+ breast cancer, especially in drug-resistant and tumorigenic cells.
  • The findings highlight GPR110's significant role in promoting tumor cell growth and dissemination in HER2+ BC.
  • GPR110 represents a promising therapeutic target for overcoming resistance and treating advanced HER2+ breast cancer.
Keywords:
Breast cancerDrug resistanceDrug targetsGPR110HER2Tumorigenesis

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