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Title: Binding optimization through coordination chemistry: CXCR4 chemokine receptor antagonists from ultrarigid metal complexes
Authors: Khan, Abid ×
Nicholson, Gary
Greenman, John
Madden, Leigh
McRobbie, Graeme
Pannecouque, Christophe
De Clercq, Erik
Ullom, Robert
Maples, Danny L
Maples, Randall D
Silversides, Jon D
Hubin, Timothy J
Archibald, Stephen J #
Issue Date: Mar-2009
Publisher: American Chemical Society
Series Title: Journal of the American Chemical Society vol:131 issue:10 pages:3416-3417
Abstract: A new copper(II) containing bis-macrocyclic CXCR4 chemokine receptor antagonist is shown to have improved binding properties to the receptor protein in comparison to the drug AMD3100 (Plerixafor, Mozobil). The interaction of the metallodrug has been optimized by using ultrarigid chelator units that offer an equatorial site for coordination to the amino acid side chains of the protein. Binding competition assays with anti-CXCR4 antibodies show that the new compound stays bound longer and it has improved anti-HIV potency in vitro (EC(50) = 4.3 nM). X-ray structural studies using acetate as a model for carboxylate amino acid side chains indicate the nature of the coordination interaction.
URI: 
ISSN: 0002-7863
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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