Inhibitors of Serine Esterases

Serine hydrolases are enzymes that play a key role in diverse physiological systems. They all use a serine side-chain hydroxy group as a nucleophile in their enzymatic reaction. In contrast to the serine proteases of the trypsin/elastase family discussed above, the two esterases discussed here belong to a different mechanistic class that shares no sequence homology or structural similarity. Lipases digest nutritional fat triglycerides and acetylcholinesterase degrades the synaptic neurotransmitter, acetylcholine. 

The following study has been undertaken in order to elucidate the distinctly different mode of action of the two esterases compared to trypsin, to rationalize structure-activity relationships of known inhibitors, and to form a basis for future ligand design projects. 

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