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

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Author

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

Summary, in English

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.

Department/s

Publishing year

2006

Language

English

Pages

6638-6641

Publication/Series

Journal of Medicinal Chemistry

Volume

49

Issue

23

Document type

Journal article

Publisher

The American Chemical Society (ACS)

Topic

  • Cell and Molecular Biology

Status

Published

Research group

  • Lung Biology

ISBN/ISSN/Other

  • ISSN: 1520-4804