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Pharmacological characterization of a small‐molecule agonist for the chemokine receptor CXCR3
Author(s) -
Scholten DJ,
Canals M,
Wijtmans M,
de Munnik S,
Nguyen P,
Verzijl D,
de Esch IJP,
Vischer HF,
Smit MJ,
Leurs R
Publication year - 2012
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.2011.01648.x
Subject(s) - cxcr3 , chemokine receptor , agonist , microbiology and biotechnology , chemistry , allosteric regulation , chemotaxis , cxcl11 , g protein coupled receptor , c c chemokine receptor type 6 , xcl2 , receptor , biology , pharmacology , biochemistry , chemokine
The chemokine receptor CXCR3 is a GPCR found predominantly on activated T cells. CXCR3 is activated by three endogenous peptides; CXCL9, CXCL10 and CXCL11. Recently, a small-molecule agonist, VUF10661, has been reported in the literature and synthesized in our laboratory. The aim of the present study was to provide a detailed pharmacological characterization of VUF10661 by comparing its effects with those of CXCL11.

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