Related Experiment Video

Updated: Oct 3, 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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G Protein-Coupled Receptors in Osteoarthritis

Fanhua Wang1, Mingyao Liu2, Ning Wang3

  • 1Yangzhi Rehabilitation Hospital (Shanghai Sunshine Rehabilitation Center), Tongji University School of Medicine, Shanghai, China.

Frontiers in Endocrinology
|February 14, 2022
PubMed

Insights

Osteoarthritis therapies targeting G-protein coupled receptors (GPCRs) show promise for managing cartilage degeneration and pain. This review explores GPCRs as therapeutic targets for osteoarthritis, highlighting challenges and potential strategies.

Area of Science:

  • Rheumatology and Pharmacology
  • Molecular Biology and Biochemistry

Background:

  • Osteoarthritis (OA) is a prevalent chronic joint disease causing significant disability.
  • Current OA treatments lack disease-modifying capabilities.
  • G-protein coupled receptors (GPCRs) play critical roles in OA pathogenesis, including cartilage breakdown, bone changes, and pain.

Purpose of the Study:

  • To review pathophysiological processes in OA targeted by GPCRs.
  • To examine preclinical and clinical data related to GPCRs in OA.
  • To identify promising GPCR targets for novel OA therapies.

Main Methods:

  • Literature review of scientific publications and clinical trial data.
  • Analysis of the role of various GPCRs in OA.
  • Identification of therapeutic strategies targeting specific GPCRs.

Main Results:

  • GPCRs are implicated in OA cartilage degeneration, subchondral bone sclerosis, and chronic pain.
  • Examples of therapeutic GPCR targets include receptors for cannabinoids, hormones, prostaglandins, fatty acids, adenosine, and chemokines.
  • Preclinical and clinical data support the potential of targeting these GPCRs.

Conclusions:

  • GPCRs represent a significant area for developing disease-modifying OA therapies.
  • Targeting specific GPCRs offers potential strategies to combat OA progression and associated pain.
  • Further research and development are needed to overcome challenges in translating these therapies to clinical practice.
Keywords:
G protein-coupled receptorsOA paincartilage degradationclinical trialsosteoarthritis

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