Chemokines are a family of small basic proteins which induce the directed migration of cells, notably leucocytes, by binding to specific GPCRs (G-protein-coupled receptors). Both chemokines and their receptors have been implicated in a host of clinically important diseases, leading to the notion that antagonism of the chemokine–chemokine receptor network may be therapeutically advantageous. Consequently, considerable effort has been put into the development of small-molecule antagonists of chemokine receptors and several such compounds have been described in the literature. One curious by-product of this activity has been the description of several small-molecule agonists of the receptors, which are typically discovered following the optimization of lead antagonists. In this review we discuss these findings and conclude that these small-molecule agonists might be exploited to further our understanding of the molecular mechanisms by which chemokine receptors are activated.
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August 2007
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Conference Article|
July 20 2007
Unravelling the mechanisms underpinning chemokine receptor activation and blockade by small molecules: a fine line between agonism and antagonism?
E. Wise;
E. Wise
1
1Leukocyte Biology Section, NHLI Division, Faculty of Medicine, Imperial College London, South Kensington Campus, London SW7 2AZ, U.K.
1To whom correspondence should be addressed (email e.wise@imperial.ac.uk)
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J.E. Pease
J.E. Pease
1Leukocyte Biology Section, NHLI Division, Faculty of Medicine, Imperial College London, South Kensington Campus, London SW7 2AZ, U.K.
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Publisher: Portland Press Ltd
Received:
April 02 2007
Online ISSN: 1470-8752
Print ISSN: 0300-5127
© The Authors Journal compilation © 2007 Biochemical Society
2007
Biochem Soc Trans (2007) 35 (4): 755–759.
Article history
Received:
April 02 2007
Citation
E. Wise, J.E. Pease; Unravelling the mechanisms underpinning chemokine receptor activation and blockade by small molecules: a fine line between agonism and antagonism?. Biochem Soc Trans 1 August 2007; 35 (4): 755–759. doi: https://doi.org/10.1042/BST0350755
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