Pharmacological Characterisation of a Small-Molecule Agonist for the Chemokine Receptor CXCR3

D.J. Scholten, M. Canals, M. Wijtmans, S.M. de Munnik, D Nguyen, D. Verzijl, I.J.P. de Esch, H.F. Vischer, M.J. Smit, R. Leurs

Research output: Contribution to JournalArticleAcademicpeer-review

Abstract

BACKGROUND AND PURPOSE 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. EXPERIMENTAL APPROACH Agonistic properties of VUF10661 were assessed in a chemotaxis assay with murine L1.2 cells transiently transfected with cDNA encoding the human CXCR3 receptor and in binding studies, with [
Original languageEnglish
Pages (from-to)898-911
JournalBritish Journal of Pharmacology
Volume166
Issue number3
DOIs
Publication statusPublished - 2011

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