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FLAP inhibitors for the treatment of inflammatory diseases

Sampson, A.P. (2009) FLAP inhibitors for the treatment of inflammatory diseases Current Opinion in Investigational Drugs, 10, (11), pp. 1163-1172. (PMID:19876784).

Record type: Article


Leukotrienes are lipid inflammatory mediators that are implicated in asthma, COPD, arthritis, cardiovascular disease and cancer. Leukotriene synthesis requires 5-lipoxygenase activating protein (FLAP), which acts as a scaffolding protein for the assembly of other enzymes involved in the leukotriene synthetic pathway occurring at the nuclear envelope of leukocytes. By blocking the formation of both leukotriene B4 and the cysteinyl leukotrienes (ie, LTC4 , LTD4 and LTE4), FLAP inhibitors act as broad-spectrum leukotriene-modifier drugs that may have a wide range of therapeutic applications. FLAP inhibitors such as MK-886, MK-0591 and veliflapon (BAY-X-1005, DG-031) demonstrated promise in clinical trials with patients with inflammatory diseases in the mid 1990 s, but, unlike the 'lukast' class of cysteinyl-leukotriene receptor antagonists, these compounds were not brought to market. The elucidation of the 3D structure of FLAP has enabled novel compound development, and several FLAP inhibitors including 2190914 (AM-103) and GSK-2190915 (both under development by GlaxoSmithKline plc) have entered phase II trials for the treatment of inflammatory disease, including asthma.

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Published date: November 2009


Local EPrints ID: 73113
ISSN: 1472-4472
PURE UUID: 8601f0d6-154b-4741-9ce4-0cc6cfea45aa

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Date deposited: 02 Mar 2010
Last modified: 18 Jul 2017 23:51

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