Related Experiment Video

Updated: Nov 22, 2025

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators

Published on: February 20, 2018

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The current status of anti-GPCR drugs against different cancers

Sana Usman1, Maria Khawer2, Shazia Rafique2

  • 1Centre for Applied Molecular Biology, 87-West Canal Bank Road Thokar Niaz Baig, University of the Punjab, Lahore, Pakistan.

Journal of Pharmaceutical Analysis
|January 11, 2021
PubMed

Insights

G protein-coupled receptors (GPCRs) are key targets for cancer drug discovery. This review explores GPCRs' role in tumor development and metastasis, highlighting therapeutic strategies and challenges.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • G protein-coupled receptors (GPCRs) are crucial drug targets for various diseases.
  • GPCRs are activated by diverse ligands like hormones, peptides, ions, and small molecules.
  • Specific GPCRs are implicated in tumorgenicity due to mutations or altered expression.

Purpose of the Study:

  • To review recent advances in understanding GPCR involvement in cancer development.
  • To discuss strategies for manipulating GPCRs to inhibit tumor growth and metastasis.
  • To provide insights into current GPCR-targeted cancer therapy, progress, and challenges.

Main Methods:

  • Literature review of recent scientific advances.
  • Analysis of molecular genetics findings linking GPCRs to cancer.
  • Discussion of therapeutic approaches targeting GPCRs in oncology.

Main Results:

  • GPCRs play a significant role in the development and progression of various human cancers.
  • Targeting GPCRs offers a promising avenue for anticancer drug development.
  • Understanding GPCR mechanisms is vital for effective cancer treatment.

Conclusions:

  • GPCRs are critical targets for novel anticancer therapies.
  • Further research is needed to overcome challenges in developing GPCR-based cancer drugs.
  • GPCR-targeted therapies hold potential for treating diverse human cancers.
Keywords:
Anticancer therapyCLLColon cancerGPCRsMelanomaPancreatic cancerProstate cancer

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