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Updated: Jun 23, 2026

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
Chemokine receptor antagonists: part 2.
1Faculty of Medicine National Heart and Lung Institute, Imperial College of Science, Technology & Medicine, Leukocyte Biology Section, London, UK. j.pease@imperial.ac.uk
This review covers chemokine receptor antagonists, focusing on CCR5, CCR8, CCR9, CXCR3, and CXCR4. While maraviroc (CCR5 inhibitor) is approved for AIDS, many antagonists have failed, prompting interest in promiscuous receptor antagonists.
Area of Science:
- Medicinal Chemistry
- Pharmacology
- Immunology
Background:
- Previous review covered CC chemokine receptors CCR1, CCR2, CCR3, and CCR4 antagonists.
- This review focuses on antagonists for CCR5, CCR8, CCR9, CXCR3, and CXCR4.
Purpose of the Study:
- To conclude a two-part review on chemokine receptor antagonists.
- To describe antagonists for specific chemokine receptors (CCR5, CCR8, CCR9, CXCR3, CXCR4) and promiscuous antagonists.
Main Methods:
- Literature review of existing research on chemokine receptor antagonists.
- Analysis of clinical trial outcomes and therapeutic successes/failures.
Main Results:
- Maraviroc, a CCR5 antagonist, is the only approved drug for treating AIDS.
- Numerous chemokine receptor antagonists have failed in clinical trials.
- Promiscuous receptor antagonists are being explored as an alternative therapeutic strategy.
Conclusions:
- Chemokine receptor antagonists have shown limited success in therapeutic applications.
- The development of effective chemokine receptor antagonists remains challenging.
- Exploring promiscuous antagonists may offer a new avenue for therapeutic development.
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