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Platelet-activating factor (PAF) is a pro-inflammatory phospholipid mediator that is rapidly synthesized by lyso-PAF acetyltransferase (lyso-PAFAT) in response to extracellular stimuli. Two types of lyso-PAFAT have been identified: lysophosphatidylcholine acyltransferase (LPCAT)1, which is mostly expressed in the lungs, and LPCAT2, which is expressed in inflammatory cells. TSI-01 is a selective inhibitor of LPCAT2 (IC50s = 0.47 versus 3.02 µM for human LPCAT2 and LPCAT1, respectively).1 At 60 µM it was shown to suppress PAF biosynthesis in mouse peritoneal macrophages stimulated with a calcium ionophore.1
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1. Selective inhibitors of a PAF biosynthetic enzyme lysophosphatidylcholine acyltransferase 2. J. Lipid Res. 55(7), 1386-1396 (2014).
ATGL is a biosynthetic enzyme for fatty acid esters of hydroxy fatty acids. Nature (2021).