Article
Identification of overlapping but differential binding sites for the high-affinity CXCR3 antagonists NBI-74330 and VUF11211.
Molecular pharmacology - 1 Jan 2014
Scholten Danny J, Roumen Luc, Wijtmans Maikel, Verkade-Vreeker Marlies C A, Custers Hans, Lai Michael, de Hooge Daniela, Canals Meritxell, de Esch Iwan J P, Smit Martine J, de Graaf Chris, Leurs Rob
Abstract excerpt
CXC chemokine receptor CXCR3 and/or its main three ligands CXCL9, CXCL10, and CXCL11 are highly upregulated in a variety of diseases. As such, considerable efforts have been made to develop small-molecule receptor CXCR3 antagonists, yielding distinct chemical classes of antagonists blocking binding and/or function of CXCR3 chemokines. Although it is suggested that these compounds bind in an allosteric fashion,...
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