|
rdf:type |
|
|
lifeskim:mentions |
umls-concept:C0021368,
umls-concept:C0205177,
umls-concept:C0205314,
umls-concept:C0205531,
umls-concept:C0226896,
umls-concept:C0243076,
umls-concept:C0442027,
umls-concept:C0596020,
umls-concept:C0679622,
umls-concept:C0700624,
umls-concept:C1415238,
umls-concept:C1441547,
umls-concept:C1527415
|
|
pubmed:issue |
23
|
|
pubmed:dateCreated |
2006-12-12
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|
pubmed:abstractText |
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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|
pubmed:language |
eng
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|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Nov
|
|
pubmed:issn |
0022-2623
|
|
pubmed:author |
|
|
pubmed:issnType |
Print
|
|
pubmed:day |
16
|
|
pubmed:volume |
49
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
6638-41
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|
pubmed:meshHeading |
pubmed-meshheading:17154491-Acetic Acids,
pubmed-meshheading:17154491-Animals,
pubmed-meshheading:17154491-Anti-Allergic Agents,
pubmed-meshheading:17154491-Asthma,
pubmed-meshheading:17154491-Binding, Competitive,
pubmed-meshheading:17154491-Biological Availability,
pubmed-meshheading:17154491-Eosinophils,
pubmed-meshheading:17154491-Fluorescence Resonance Energy Transfer,
pubmed-meshheading:17154491-Humans,
pubmed-meshheading:17154491-Inflammation,
pubmed-meshheading:17154491-Mice,
pubmed-meshheading:17154491-Models, Molecular,
pubmed-meshheading:17154491-Pyrazoles,
pubmed-meshheading:17154491-Radioligand Assay,
pubmed-meshheading:17154491-Rats,
pubmed-meshheading:17154491-Receptors, Immunologic,
pubmed-meshheading:17154491-Receptors, Prostaglandin,
pubmed-meshheading:17154491-Stereoisomerism,
pubmed-meshheading:17154491-Structure-Activity Relationship,
pubmed-meshheading:17154491-Th2 Cells
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|
pubmed:year |
2006
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|
pubmed:articleTitle |
Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits.
|
|
pubmed:affiliation |
7TM Pharma, Fremtidsvej 3, DK-2970 Hørsholm, Denmark. ulven@chem.sdu.dk
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|
pubmed:publicationType |
Journal Article,
In Vitro
|
