Allosteric modulation of chemokine receptors

Nuska Tschammer, Arthur Christopoulos, Terry Kenakin

Research output: Chapter in Book/Report/Conference proceedingChapter (Book)Researchpeer-review

3 Citations (Scopus)


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.
Original languageEnglish
Title of host publicationChemokines: Chemokines and Their Receptors in Drug Discovery
EditorsNuska Tschammer
Place of PublicationCham Switzerland
Number of pages31
ISBN (Print)9783319140599
Publication statusPublished - 2015

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