Monocyte and macrophage selective anti-inflammatory kinase inhibitors

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.