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Identification and characterisation of new inhibitors for the human hematopoietic prostaglandin D 2 synthase

Weber, Jane E; Oakley, Aaron; Christ, Angelika N; Clark, Alan G; Hayes, John D; Hall, Rhonda; Hume, David A; Board, Philip; Smythe, Mark L; Flanagan, Jack U

Description

Prostaglandin D2 synthesised by the hematopoietic prostaglandin D2 synthase has a pro-inflammatory effect in allergic asthma, regulating many hallmark characteristics of the disease. Here we describe identification of hematopoietic prostaglandin D2 synthase inhibitors including cibacron blue, bromosulfophthalein and ethacrynic acid. Expansion around the drug-like ethacrynic acid identified a novel inhibitor, nocodazole, and a fragment representing its aromatic core. Nocodazole binding was...[Show more]

CollectionsANU Research Publications
Date published: 2010
Type: Journal article
URI: http://hdl.handle.net/1885/55961
Source: European Journal of Medicinal Chemistry
DOI: 10.1016/j.ejmech.2009.10.025

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