Related Experiment Video

Updated: Jan 17, 2026

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

9.4K

G Protein-Coupled Receptor Signaling: Implications and Therapeutic Development Advances in Cancers

Inamu Rashid Khan1, Sana Khurshid2, Saud Almawash3

  • 1Department of Zoology Central University of Kashmir Ganderbal Kashmir India.

Medcomm
|September 19, 2025
PubMed

Insights

G protein-coupled receptors (GPCRs) are key membrane proteins involved in cancer. Understanding their complex signaling pathways, particularly biased signaling, is crucial for developing targeted cancer therapies.

Area of Science:

  • Molecular Biology
  • Cellular Biology
  • Pharmacology

Background:

  • G protein-coupled receptors (GPCRs) are a large class of membrane proteins mediating cellular responses.
  • GPCRs regulate vital physiological functions and are implicated in various diseases, including cancer.
  • Abnormal GPCR signaling in tumors promotes carcinogenesis by influencing immune evasion, proliferation, and therapeutic resistance.

Purpose of the Study:

  • To review the complexity of GPCRs and their role in cancer signaling.
  • To focus on differential pathway activation by G proteins and β-arrestin.
  • To explore targeted modulation of GPCR signaling for cancer treatment.

Main Methods:

  • Literature review of GPCR structure-function relationships.
  • Analysis of GPCR-biased signaling mechanisms.
  • Examination of emerging technologies for GPCR targeting.

Main Results:

  • GPCRs' seven-transmembrane structure facilitates diverse signaling networks.
  • Pathway-specific GPCR activation and biased ligand discovery are critical research areas.
  • Targeted modulation of GPCR signaling pathways shows therapeutic potential in cancer.

Conclusions:

  • Understanding GPCR-biased signaling offers insights into cancer biology.
  • Emerging technologies like aptamers, PROTACs, and nanobodies enable precise GPCR targeting.
  • Modulating GPCR signaling pathways may lead to more effective cancer therapies.
Keywords:
GPCRsbiascancerdiseasessignalingtherapeutics

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