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Updated: Dec 27, 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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Targeting G protein-coupled receptors in cancer therapy

Surinder M Soond1, Andrey A Zamyatnin2

  • 1Institute of Molecular Medicine, Sechenov First Moscow State Medical University, Moscow, Russian Federation.

Advances in Cancer Research
|February 25, 2020
PubMed

Insights

Research into G protein-coupled receptors (GPCRs) is yielding new therapeutic strategies. Elucidating GPCR crystal structures is accelerating the development of drugs targeting these key signaling proteins for various diseases.

Area of Science:

  • Pharmacology
  • Molecular Biology
  • Biochemistry

Background:

  • G protein-coupled receptors (GPCRs) are crucial cell surface receptors involved in numerous physiological processes.
  • Dysregulation of GPCR signaling is implicated in various diseases, including cancer.
  • Therapeutic intervention targeting GPCRs has been challenging due to their complexity.

Purpose of the Study:

  • To review recent advancements in developing therapeutics targeting GPCRs.
  • To highlight the role of GPCR structural biology in drug discovery.
  • To explore strategies for targeting specific GPCR domains and associated molecules.

Main Methods:

  • Elucidation of GPCR crystal structures to understand protein dynamics.
  • Development of therapeutics targeting extracellular and intracellular domains.
  • Investigation of ligands and auxiliary proteins interacting with GPCRs.

Main Results:

  • Recent studies defining GPCR protein dynamics through crystal structure elucidation have gained momentum.
  • This structural information facilitates the design of targeted therapeutics.
  • GPCR-derived signaling pathways are emerging as important therapeutic targets.

Conclusions:

  • Structural insights into GPCRs are crucial for developing effective therapeutics.
  • Targeting specific receptor domains and associated molecules offers promising therapeutic avenues.
  • GPCR signaling pathways represent a significant, largely untapped resource for drug development.
Keywords:
CancerGPCRGRKHIPPOLPAPARS1PTAZTherapeuticsYAPβ-Arrestin

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