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Pathological changes in GPCR signal organisation: Opportunities for targeted therapies for triple negative breast

Terrance Lam1, Chantel Mastos1, Erica K Sloan1

  • 1Drug Discovery Biology Theme, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia.

Pharmacology & Therapeutics
|December 13, 2022
PubMed

Insights

Triple negative breast cancer (TNBC) progresses due to the β2-adrenoceptor, a G protein-coupled receptor (GPCR). Targeting GPCRs in unique cellular locations offers new therapeutic strategies for TNBC.

Area of Science:

  • Oncology
  • Cell Biology
  • Pharmacology

Background:

  • Triple negative breast cancer (TNBC) has a poor prognosis and limited targeted therapies.
  • G protein-coupled receptors (GPCRs), like the β2-adrenoceptor, are emerging as potential therapeutic targets.
  • Understanding TNBC signaling pathways is crucial for developing effective treatments.

Purpose of the Study:

  • To investigate the role of the β2-adrenoceptor in TNBC progression and invasion.
  • To elucidate the unique signaling pathway activated by β2-adrenoceptor in aggressive TNBC cells.
  • To explore the therapeutic potential of targeting GPCRs in aberrant cellular locations.

Main Methods:

  • Analysis of signaling pathways in TNBC tumor cells.
  • Investigating the function of β2-adrenoceptor in response to stress.
  • Studying GPCR organization and localization within tumor cells.

Main Results:

  • The β2-adrenoceptor accelerates TNBC progression under stress.
  • A unique signaling pathway activated by β2-adrenoceptor drives aggressive TNBC cell invasion.
  • Evidence suggests altered GPCR organization in tumor cells, leading to unique cellular responses.

Conclusions:

  • The β2-adrenoceptor is a key driver of TNBC progression and invasion.
  • Aberrant GPCR localization in tumor cells presents novel therapeutic opportunities.
  • Targeted anti-cancer GPCR drugs could offer improved efficacy and reduced side effects.
Keywords:
Compartmentalised signallingG protein-coupled receptorsIntracellular receptorsTriple negative breast cancer

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