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Chemokine and Cytokine Modulators

  1. Maria Elena Fuentes,
  2. Tara Mirzadegan,
  3. Robert S. Wilhelm

Published Online: 15 JAN 2003

DOI: 10.1002/0471266949.bmc062

Burger's Medicinal Chemistry and Drug Discovery

Burger's Medicinal Chemistry and Drug Discovery

How to Cite

Fuentes, M. E., Mirzadegan, T. and Wilhelm, R. S. 2003. Chemokine and Cytokine Modulators. Burger's Medicinal Chemistry and Drug Discovery. 119–192.

Author Information

  1. Roche Bioscience, Palo Alto, California, USA

Publication History

  1. Published Online: 15 JAN 2003


The ability to respond to exogenous stimuli is a key characteristic in the survival of multicellular organisms. Both chemokines and cytokines participate in this process with different mechanisms. Chemokines are mostly involved in chemoattraction of different cell types to inflamed tissues. Cytokines, on the other hand, regulate gene expression in a wide variety of cell types. Both types of molecules are mostly inducible, although some participate in homeostatic processes. Chemokines exert their action through the activation of seven-transmembrane spanning receptors also called G-protein-coupled receptors. Cytokine receptors are usually formed of two or more single-spanning membrane subunits and phosphorylation is crucial in the signaling cascade. Because of the nature of the receptors, significant information is available regarding attempts to block chemokine receptors with small molecule antagonists. The situation is quite different for cytokine receptors, in which most of the antagonists described so far are either receptor antibodies or soluble receptors. In this chapter we summarize data available for both families.


  • cytokines;
  • chemokines;
  • cytokine receptors;
  • chemokine receptors;
  • GPCR;
  • inflammation