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Issue 9, 2012
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Monocyte and macrophage selective anti-inflammatory kinase inhibitors

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Abstract

Appending appropriate esters to anti-inflammatory compounds leads to monocyte/macrophage selectivity. This has been demonstrated in p38α MAP kinase in which we observe differential inhibition of phosphorylation of the substrate MAPKAPK2 in stimulated cells. This selectivity is due to differential expression of carboxylesterases within the cells, which cause the active form of the compounds to accumulate with the cells.

Graphical abstract: Monocyte and macrophage selective anti-inflammatory kinase inhibitors

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Publication details

The article was received on 09 Feb 2012, accepted on 16 Jun 2012 and first published on 20 Jun 2012


Article type: Concise Article
DOI: 10.1039/C2MD20158E
Med. Chem. Commun., 2012,3, 1070-1076

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    Monocyte and macrophage selective anti-inflammatory kinase inhibitors

    M. H. Charlton, D. H. Brotherton, J. Owen, V. L. Clark, R. J. Testar, S. J. Davies and D. F. C. Moffat, Med. Chem. Commun., 2012, 3, 1070
    DOI: 10.1039/C2MD20158E

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