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Discovery of a Novel Series of CRTH2 (DP2) Receptor Antagonists Devoid of Carboxylic Acids.
- Stefano Crosignani, C. Jorand-Lebrun, +19 authors Zoë Johnson
- ACS medicinal chemistry letters
- 17 October 2011
Antagonism of the CRTH2 receptor represents a very attractive target for a variety of allergic diseases. Most CRTH2 antagonists known to date possess a carboxylic acid moiety, which is essential for… Expand
Functional analysis and transcriptional output of the Göttingen minipig genome
BackgroundIn the past decade the Göttingen minipig has gained increasing recognition as animal model in pharmaceutical and safety research because it recapitulates many aspects of human physiology… Expand
Discovery of potent, selective, and orally bioavailable alkynylphenoxyacetic acid CRTH2 (DP2) receptor antagonists for the treatment of allergic inflammatory diseases.
- Stefano Crosignani, Adeline Prêtre, +18 authors Z. Johnson
- Chemistry, Medicine
- Journal of medicinal chemistry
- 3 October 2011
New phenoxyacetic acid antagonists of CRTH2 are described. Following the discovery of a hit compound by a focused screening, high protein binding was identified as its main weakness. Optimization… Expand