Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits
(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.
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/1298261
- author
- 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
- organization
- publishing date
- 2006
- 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}}, }