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

    Research output: Contribution to JournalArticleAcademicpeer-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 languageEnglish
    Pages (from-to)783-90
    JournalThe Journal of Pharmacology and Experimental Therapeutics
    Volume329
    Issue number2
    DOIs
    Publication statusPublished - 2009

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