AI Article Synopsis
- The chemokine system plays a crucial role in directing leukocytes to specific tissue locations, highlighting its importance in inflammatory responses.
- Chemokine receptors are part of the GPCR superfamily, which makes them promising targets for new drug development, yet none of the existing small molecule antagonists have proven effective in treating inflammatory diseases in clinical settings.
- This article explores the successes and failures of these chemokine receptor antagonists in clinical trials and suggests that developing drugs that target multiple chemokine receptors simultaneously may lead to more effective anti-inflammatory treatments in the future.
Article Abstract
A major function of the chemokine system is to coordinate the recruitment of leukocytes to specific locations within the tissues. The involvement of chemokine receptors in a multitude of inflammatory diseases, coupled with their belonging to the highly "druggable" GPCR superfamily, makes them excellent candidates for the development of novel drugs by the pharmaceutical industry. Despite descriptions in the literature of many specific small molecule chemokine receptor antagonists, none have yet shown efficacy in the clinical inflammatory setting. In this article, we discuss the successes and failures of chemokine receptor antagonists in the clinic and review a subset of molecules that are documented as having activity at two or more chemokine receptors. It may be that a more permissive approach, targeting several chemokine receptors with a single molecule will provide the next generation of anti-inflammatory drugs.
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| http://dx.doi.org/10.2174/156802610791561228 | DOI Listing |
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