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

doi:10.1111/j.1476-5381.2011.01648.x

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 Journal › Article › Academic › peer-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 language	English
Pages (from-to)	898-911
Journal	British Journal of Pharmacology
Volume	166
Issue number	3
DOIs	https://doi.org/10.1111/j.1476-5381.2011.01648.x
Publication status	Published - 2011

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10.1111/j.1476-5381.2011.01648.x

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title = "Pharmacological Characterisation of a Small-Molecule Agonist for the Chemokine Receptor CXCR3",

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 [",

author = "D.J. Scholten and M. Canals and M. Wijtmans and {de Munnik}, S.M. and D Nguyen and D. Verzijl and {de Esch}, I.J.P. and H.F. Vischer and M.J. Smit and R. Leurs",

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doi = "10.1111/j.1476-5381.2011.01648.x",

language = "English",

volume = "166",

pages = "898--911",

journal = "British Journal of Pharmacology",

issn = "0007-1188",

publisher = "Wiley-Blackwell",

number = "3",

}

Pharmacological Characterisation of a Small-Molecule Agonist for the Chemokine Receptor CXCR3. / Scholten, D.J.; Canals, M.; Wijtmans, M.; de Munnik, S.M.; Nguyen, D; Verzijl, D.; de Esch, I.J.P.; Vischer, H.F.; Smit, M.J.; Leurs, R.

In: British Journal of Pharmacology, Vol. 166, No. 3, 2011, p. 898-911.

Research output: Contribution to Journal › Article › Academic › peer-review

TY - JOUR

T1 - Pharmacological Characterisation of a Small-Molecule Agonist for the Chemokine Receptor CXCR3

AU - Scholten, D.J.

AU - Canals, M.

AU - Wijtmans, M.

AU - de Munnik, S.M.

AU - Nguyen, D

AU - Verzijl, D.

AU - de Esch, I.J.P.

AU - Vischer, H.F.

AU - Smit, M.J.

AU - Leurs, R.

PY - 2011

Y1 - 2011

N2 - 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 [

AB - 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 [

U2 - 10.1111/j.1476-5381.2011.01648.x

DO - 10.1111/j.1476-5381.2011.01648.x

M3 - Article

VL - 166

SP - 898

EP - 911

JO - British Journal of Pharmacology

JF - British Journal of Pharmacology

SN - 0007-1188

IS - 3

ER -

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

Abstract

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