Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits

Trond Ulven, Jean-Marie Receveur, Marie Grimstrup, Oystein Rist, Thomas M Frimurer, Lars-Ole Gerlach, Jesper Mosolff Mathiesen, Evi Kostenis, Lena Uller, Thomas Hogberg

Research output: Contribution to journalArticlepeer-review

Abstract

Hits from an in silico derived focused library for CRTH2 were transformed into highly selective antagonists with favorable ADME properties. Oral administration of 4-bromo-2-(1-phenyl-1H-pyrazole-4-carbonyl)phenoxyacetic acid (19) inhibited peribronchial eosinophilia and mucus cell hyperplasia in a mouse model of allergic asthma, supporting the therapeutic potential of this novel compound class. In addition, this selective pharmacological tool compound provides further evidence for CRTH2 as a relevant therapeutic target for treatment of Th2- and eosinophil-related inflammation.
Original languageEnglish
Pages (from-to)6638-6641
JournalJournal of Medicinal Chemistry
Volume49
Issue number23
DOIs
Publication statusPublished - 2006

Subject classification (UKÄ)

  • Cell and Molecular Biology

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