Abstract
| Original language | English |
|---|---|
| Title of host publication | Chemokines: Chemokines and Their Receptors in Drug Discovery |
| Editors | Nuska Tschammer |
| Place of Publication | Cham Switzerland |
| Publisher | Springer |
| Pages | 87-117 |
| Number of pages | 31 |
| ISBN (Print) | 9783319140599 |
| DOIs | |
| Publication status | Published - 2015 |
Cite this
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Allosteric modulation of chemokine receptors. / Tschammer, Nuska; Christopoulos, Arthur; Kenakin, Terry.
Chemokines: Chemokines and Their Receptors in Drug Discovery. ed. / Nuska Tschammer. Cham Switzerland : Springer, 2015. p. 87-117.Research output: Chapter in Book/Report/Conference proceeding › Chapter (Book) › Research › peer-review
TY - CHAP
T1 - Allosteric modulation of chemokine receptors
AU - Tschammer, Nuska
AU - Christopoulos, Arthur
AU - Kenakin, Terry
PY - 2015
Y1 - 2015
N2 - 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.
AB - 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.
UR - http://link.springer.com.ezproxy.lib.monash.edu.au/content/pdf/10.1007%2F7355_2014_82.pdf
U2 - 10.1007/7355_2014_82
DO - 10.1007/7355_2014_82
M3 - Chapter (Book)
SN - 9783319140599
SP - 87
EP - 117
BT - Chemokines: Chemokines and Their Receptors in Drug Discovery
A2 - Tschammer, Nuska
PB - Springer
CY - Cham Switzerland
ER -