Volume 14 of the series Topics in Medicinal Chemistry pp 87-117


Allosteric Modulation of Chemokine Receptors

  • Nuska TschammerAffiliated withDepartment of Chemistry and Pharmacy, Medicinal Chemistry, Emil Fischer Center, Friedrich Alexander University Email author 
  • , Arthur ChristopoulosAffiliated withDepartment of Pharmacology, Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University
  • , Terry KenakinAffiliated withDepartment of Pharmacology, University of North Carolina School of Medicine

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A central role of chemokines and their receptors in inflammatory processes has spurred numerous screening campaigns dedicated to the search for chemokine-receptor antagonists, which largely failed to deliver drugs for the treatment of inflammatory diseases. The quest for effective chemokine-receptor drug candidates thus continues, and the concept of allosteric targeting of the receptors may be the way forward. In this review, the complex allosteric mechanisms by which the functions of chemokines and their receptors are fine-tuned will be discussed and their impact on preclinical drug discovery presented. The opportunities and challenges of bench-to-clinic approaches are elucidated. We propose that while allosteric modulation of chemokine receptors adds a level of complexity to analyses and approaches to drug discovery, it also introduces a tremendous capacity for pharmacologic control of this physiological system for therapeutic advantage.