Synthesis of an acyl-acyl carrier protein synthetase inhibitor to study fatty acid recycling.

摘要: Fatty acids are essential to most organisms and made endogenously by the fatty acid synthase (FAS). FAS is an attractive target for antibiotics many inhibitors in clinical development. However, some gram-negative bacteria harbor enzyme known as acyl-acyl carrier protein synthetase (AasS), which allows them scavenge from environment shuttle into ultimately lipids. The ability of AasS recycle may help pathogenic circumvent inhibition. We therefore set out design synthesize inhibitor test its effectiveness on Vibrio harveyi, well studied date, cholerae, a model. C10-AMS [5'-O-(N-decanylsulfamoyl)adenosine], mimics tightly bound acyl-AMP reaction intermediate, was able effectively inhibit catalytic activity vitro. Additionally, stopped cholerae media survive when endogenous inhibited with cerulenin. can be used study recycling other more enzymes continue annotated provides platform potential antibiotic