5fv4 | pdb_00005fv4
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Structural highlights
FunctionEST1_PIG Involved in the detoxification of xenobiotics and in the activation of ester and amide prodrugs. Active towards triacylglycerides containing short-chain fatty acids from C2 to C6, and 1(3)-monoacylglycerols containing fatty acids from C2 to C12. Inactive on long-chain triacylglycerols and diacylglycerol. Hydrolyzes aromatic and alkyl esters and vitamin A acetate. The hydrolysis rate depends upon the amino acid promoiety and the esterification site of the prodrug. Aromatic promoieties are favored, highest rates are observed with phenylalanyl progdrugs, hydrolysis of valyl and isoleucyl prodrugs is less efficient. With floxuridine prodrugs, activity is higher on 5' monoesters than on 3' monoesters. With gemcitabine prodrugs, activity is higher on 3' monoesters than on 5' monoesters.[1] [2] [3] References
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This page was last modified 13:28, 26 July 2023.