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Content material: part 1. Arachidonic acid cascade -- part 2. Kinases -- part three. GPCRs -- part four. Sphingolipids -- part five. Steroid hormone receptors
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1–7 A current classiﬁcation scheme divides the PLA2s into 12 groups (I–XII) with diﬀerent subgroups based on their structures, enzymatic characteristics and subcellular distribution. Alternatively, the PLA2s can be ordered into such enzymes that utilize a catalytic histidine and in enzymes that have a catalytic serine. The small secretory PLA2s (sPLA2), which require millimolar Ca21 for the phospholipid cleavage, belong to the ﬁrst category. 6 The serine branch of the PLA2 family composes larger enzymes that do not contain a Ca21 in the active site.
COX-2-derived formation of 6-keto PGF1a was not aﬀected under the same conditions in A549 cells. 176 However, introduction of long and bulky lipophilic substituents (hexyl-, octyl- or naphthyl-residues) yielded potent dual Microsomal Prostaglandin E2 Synthase-1 19 inhibitors of mPGES-1 and 5-LO. 187 PGE2 formation in LPS-stimulated whole blood was inhibited with an IC50 of 2 mM, whereas TxB2 and 6-keto PGF1a formation were not signiﬁcantly reduced. ). 1 mM in cell-free assays. 1 mM). 5 mM, respectively.
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