Article
Mutation of Cys242 of human monoacylglycerol lipase disrupts balanced hydrolysis of 1- and 2-monoacylglycerols and selectively impairs inhibitor potency.
Molecular pharmacology - 1 Mar 2014
Laitinen Tuomo, Navia-Paldanius Dina, Rytilahti Roosa, Marjamaa Joona J T, Kařízková Julie, Parkkari Teija, Pantsar Tatu, Poso Antti, Laitinen Jarmo T, Savinainen Juha R
Abstract excerpt
Considerable progress has been made in recent years in developing selective, potent monoacylglycerol lipase (MAGL) inhibitors. In the investigations of measures to inhibit this enzyme, less attention has been paid to improving our understanding of its catalytic mechanisms or substrate preferences. In our study, we used site-directed mutagenesis, and we show via versatile activity assays combined with molecular...
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