Bivalent Ligands Targeting Chemokine Receptor Dimerization: Molecular Design and Functional Studies

Author(s): Christopher Kent Arnatt, Yan Zhang

Journal Name: Current Topics in Medicinal Chemistry

Volume 14 , Issue 13 , 2014

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Graphical Abstract:


Increasing evidence has shown that chemokine receptors may form functional dimers with unique pharmacological profiles. A common practice to characterize such G protein-coupled receptor dimerization processes is to apply bivalent ligands as chemical probes which can interact with both receptors simultaneously. Currently, two chemokine receptor dimers have been studied by applying bivalent compounds: the CXCR4-CXCR4 homodimer and the CCR5-MOR heterodimer. These bivalent compounds have revealed how dimerization influences receptor function and may lead to novel therapeutics. Future design of bivalent ligands for chemokine receptor dimers may be aided with the recently available CXCR4 homodimer, and CCR5 monomer crystal structures by more accurately simulating chemokine receptors and their dimers.

Keywords: Bivalent ligand, CCR5, chemokine receptor, CXCR4, dimerization, GPCR, MOR.

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Article Details

Year: 2014
Published on: 03 September, 2014
Page: [1606 - 1618]
Pages: 13
DOI: 10.2174/1568026614666140827144752
Price: $65

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