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Chemokine Biology — Basic Research and Clinical Application pp 79–88Cite as

Antagonists of CXCR3: a review of current progress

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Part of the book series: Progress in Inflammation Research ((PIR))

Abstract

CXCR3 was cloned and identified as a receptor for CXCL9 and CXCL10 by Loetscher, et al., in 1996 [1], and was subsequently identified as a receptor for CXCL11 [2]. CXCL9, CXCL10 and CXCL11 are selective, potent agonists of CXCR3 (Kd 0.1–5 nM) [1]–[4]. Additional chemokines have been reported to bind to CXCR3 (e.g., CXCL13 [5] and CCL11 [6]), however the reported affinities are generally weak and the biological significance of the interactions is questionable. Similarly, the ligands for CXCR3 have been reported to be antagonists of CCR3 [7] and CCR5 [8], but high concentrations of the CXCR3 ligands are required to achieve inhibition of CCR3 or CCR5 biological functions.

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Author information

Authors and Affiliations

  1. Department of Neuroscience, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA, 94080, USA

    Tassie L. Collins

  2. Department of Chemistry, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA, 94080, USA

    Michael G. Johnson & Julio C. Medina

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  1. Tassie L. Collins
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  2. Michael G. Johnson
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  3. Julio C. Medina
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Editors and Affiliations

  1. Lilly Corporate Center, Cancer Inflammation and Cell Survival Eli Lilly and Company, Indianapolis, IN, 46285, USA

    Kuldeep Neote

  2. NitroMed, Inc., 12 Oak Park Drive, Bedford, MA, 01730, USA

    Gordon L. Letts

  3. Theodor Koch Institute, University of Bern, Freiestrasse 1, 3012, Bern, Switzerland

    Bernhard Moser

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© 2007 Birkhäuser Verlag Basel/Switzerland

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Collins, T.L., Johnson, M.G., Medina, J.C. (2007). Antagonists of CXCR3: a review of current progress. In: Neote, K., Letts, G.L., Moser, B. (eds) Chemokine Biology — Basic Research and Clinical Application. Progress in Inflammation Research. Birkhäuser Basel. https://doi.org/10.1007/978-3-7643-7437-2_6

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