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


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
Issue number2
Publication statusPublished - 2009

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