Nonpeptidergic allosteric antagonists differentially bind to the CXCR2 chemokine receptor

P. de Kruijf; J.T. van Heteren; H.D. Lim; P. Conti; M.M. van der Lee; L. Bosch; K.K. Ho; D.S. Auld; M. Ohlmeyer; M.J. Smit; J.C. Wijkmans; G.J. Zaman; R. Leurs

doi:10.1124/jpet.108.148387

Nonpeptidergic allosteric antagonists differentially bind to the CXCR2 chemokine receptor

P. de Kruijf, J.T. van Heteren, H.D. Lim, P. Conti, M.M. van der Lee, L. Bosch, K.K. Ho, D.S. Auld, M. Ohlmeyer, M.J. Smit, J.C. Wijkmans, G.J. Zaman, R. Leurs

Medicinal chemistry

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

Abstract

The chemokine receptor CXCR2 is involved in different inflammatory diseases, like chronic obstructive pulmonary disease, psoriasis, rheumatoid arthritis, and ulcerative colitis; therefore, it is considered an attractive drug target. Different classes of small CXCR2 antagonists have been developed. In this study, we selected seven CXCR2 antagonists from the diarylurea, imida-zolylpyrimide, and thiazolopyrimidine class and studied their mechanisms of action at human CXCR2. All compounds are able to displace

Original language	English
Pages (from-to)	783-90
Journal	The Journal of Pharmacology and Experimental Therapeutics
Volume	329
Issue number	2
DOIs	https://doi.org/10.1124/jpet.108.148387
Publication status	Published - 2009

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

Access to Document

10.1124/jpet.108.148387

Persistent URL (handle)

Copy link address

Cite this

de Kruijf, P., van Heteren, J. T., Lim, H. D., Conti, P., van der Lee, M. M., Bosch, L., Ho, K. K., Auld, D. S., Ohlmeyer, M., Smit, M. J., Wijkmans, J. C., Zaman, G. J., & Leurs, R. (2009). Nonpeptidergic allosteric antagonists differentially bind to the CXCR2 chemokine receptor. The Journal of Pharmacology and Experimental Therapeutics, 329(2), 783-90. https://doi.org/10.1124/jpet.108.148387

@article{313d3cc8b2904984a43fce680292a4cb,

title = "Nonpeptidergic allosteric antagonists differentially bind to the CXCR2 chemokine receptor",

abstract = "The chemokine receptor CXCR2 is involved in different inflammatory diseases, like chronic obstructive pulmonary disease, psoriasis, rheumatoid arthritis, and ulcerative colitis; therefore, it is considered an attractive drug target. Different classes of small CXCR2 antagonists have been developed. In this study, we selected seven CXCR2 antagonists from the diarylurea, imida-zolylpyrimide, and thiazolopyrimidine class and studied their mechanisms of action at human CXCR2. All compounds are able to displace",

author = "{de Kruijf}, P. and {van Heteren}, J.T. and H.D. Lim and P. Conti and {van der Lee}, M.M. and L. Bosch and K.K. Ho and D.S. Auld and M. Ohlmeyer and M.J. Smit and J.C. Wijkmans and G.J. Zaman and R. Leurs",

year = "2009",

doi = "10.1124/jpet.108.148387",

language = "English",

volume = "329",

pages = "783--90",

journal = "The Journal of Pharmacology and Experimental Therapeutics",

issn = "0022-3565",

publisher = "American Society for Pharmacology and Experimental Therapeutics",

number = "2",

}

de Kruijf, P, van Heteren, JT, Lim, HD, Conti, P, van der Lee, MM, Bosch, L, Ho, KK, Auld, DS, Ohlmeyer, M, Smit, MJ, Wijkmans, JC, Zaman, GJ & Leurs, R 2009, 'Nonpeptidergic allosteric antagonists differentially bind to the CXCR2 chemokine receptor', The Journal of Pharmacology and Experimental Therapeutics, vol. 329, no. 2, pp. 783-90. https://doi.org/10.1124/jpet.108.148387

TY - JOUR

T1 - Nonpeptidergic allosteric antagonists differentially bind to the CXCR2 chemokine receptor

AU - de Kruijf, P.

AU - van Heteren, J.T.

AU - Lim, H.D.

AU - Conti, P.

AU - van der Lee, M.M.

AU - Bosch, L.

AU - Ho, K.K.

AU - Auld, D.S.

AU - Ohlmeyer, M.

AU - Smit, M.J.

AU - Wijkmans, J.C.

AU - Zaman, G.J.

AU - Leurs, R.

PY - 2009

Y1 - 2009

N2 - The chemokine receptor CXCR2 is involved in different inflammatory diseases, like chronic obstructive pulmonary disease, psoriasis, rheumatoid arthritis, and ulcerative colitis; therefore, it is considered an attractive drug target. Different classes of small CXCR2 antagonists have been developed. In this study, we selected seven CXCR2 antagonists from the diarylurea, imida-zolylpyrimide, and thiazolopyrimidine class and studied their mechanisms of action at human CXCR2. All compounds are able to displace

AB - The chemokine receptor CXCR2 is involved in different inflammatory diseases, like chronic obstructive pulmonary disease, psoriasis, rheumatoid arthritis, and ulcerative colitis; therefore, it is considered an attractive drug target. Different classes of small CXCR2 antagonists have been developed. In this study, we selected seven CXCR2 antagonists from the diarylurea, imida-zolylpyrimide, and thiazolopyrimidine class and studied their mechanisms of action at human CXCR2. All compounds are able to displace

U2 - 10.1124/jpet.108.148387

DO - 10.1124/jpet.108.148387

M3 - Article

SN - 0022-3565

VL - 329

SP - 783

EP - 790

JO - The Journal of Pharmacology and Experimental Therapeutics

JF - The Journal of Pharmacology and Experimental Therapeutics

IS - 2

ER -

Nonpeptidergic allosteric antagonists differentially bind to the CXCR2 chemokine receptor

Abstract

UN SDGs

Access to Document

Persistent URL (handle)

Fingerprint

Cite this