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

Ulven, Trond ; Receveur, Jean-Marie ; Grimstrup, Marie ; Rist, Oystein ; Frimurer, Thomas M ; Gerlach, Lars-Ole ; Mathiesen, Jesper Mosolff ; Kostenis, Evi ; Uller, Lena LU and Hogberg, Thomas (2006) In Journal of Medicinal Chemistry 49(23). p.6638-6641
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.
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author
; ; ; ; ; ; ; ; and
organization
publishing date
type
Contribution to journal
publication status
published
subject
in
Journal of Medicinal Chemistry
volume
49
issue
23
pages
6638 - 6641
publisher
The American Chemical Society (ACS)
external identifiers
  • wos:000241894000003
  • scopus:33750978443
  • pmid:17154491
ISSN
1520-4804
DOI
10.1021/jm060657g
language
English
LU publication?
yes
id
7f634cad-043f-472f-8bc3-359da9a08b4a (old id 1298261)
date added to LUP
2016-04-04 09:56:28
date last changed
2022-04-23 22:11:10
@article{7f634cad-043f-472f-8bc3-359da9a08b4a,
  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.}},
  author       = {{Ulven, Trond and Receveur, Jean-Marie and Grimstrup, Marie and Rist, Oystein and Frimurer, Thomas M and Gerlach, Lars-Ole and Mathiesen, Jesper Mosolff and Kostenis, Evi and Uller, Lena and Hogberg, Thomas}},
  issn         = {{1520-4804}},
  language     = {{eng}},
  number       = {{23}},
  pages        = {{6638--6641}},
  publisher    = {{The American Chemical Society (ACS)}},
  series       = {{Journal of Medicinal Chemistry}},
  title        = {{Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits}},
  url          = {{http://dx.doi.org/10.1021/jm060657g}},
  doi          = {{10.1021/jm060657g}},
  volume       = {{49}},
  year         = {{2006}},
}