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Updated: Aug 14, 2026

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
The chemokine system: novel broad-spectrum therapeutic targets
1Serono Pharmaceutical Research Institute, 14 Chemin des Aulx, Geneva, Switzerland. christine.power@serono.com
Abstract:
Chemokines are cytokines that specifically direct the trafficking of immune cells in the body. They offer a novel point of therapeutic intervention, as inhibiting specific chemokines and receptors could prevent the excessive recruitment of leukocytes to sites of inflammation. This approach could be considered to act upstream of the therapies used today which, for the most part, act on the cells already at the site of inflammation. The receptors for chemokines are G-protein-coupled seven-transmembrane receptors, which are particularly tractable for the pharmaceutical industry. The search for small-molecule inhibitors of these receptors has been fruitful and the numbers of patents and, more recently, peer-reviewed publications are growing rapidly. The first clinical trial was initiated this year, so although it is too soon to be able to report these results we hope to see the outcome of this research in the near future.
Insights
Chemokines are signaling proteins that guide immune cells. Inhibiting chemokine receptors offers a new therapeutic strategy to control inflammation by blocking immune cell movement to affected areas.
Area of Science:
- Immunology
- Pharmacology
Background:
- Chemokines are cytokines crucial for immune cell trafficking.
- Their receptors are G-protein-coupled seven-transmembrane receptors, presenting pharmaceutical targets.
Purpose of the Study:
- To explore the therapeutic potential of inhibiting chemokine and chemokine receptors.
- To highlight this approach as an upstream intervention for inflammatory diseases.
Main Methods:
- Review of current research on chemokine inhibitors.
- Analysis of patent and publication trends.
- Mention of the initiation of the first clinical trial.
Main Results:
- The search for small-molecule chemokine receptor inhibitors has yielded promising results.
- There is a rapid increase in patents and peer-reviewed publications in this field.
Conclusions:
- Inhibiting chemokine pathways represents a novel therapeutic strategy for inflammatory conditions.
- Early clinical trials are underway, indicating significant therapeutic promise.
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