structure and catalytic properties of carboxylesterase isozymes involved in metabolic activation of prodrugs结构和催化性能的羧酸酯酶同功酶参与代谢激活高活性化合物.pdfVIP

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structure and catalytic properties of carboxylesterase isozymes involved in metabolic activation of prodrugs结构和催化性能的羧酸酯酶同功酶参与代谢激活高活性化合物.pdf

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structure and catalytic properties of carboxylesterase isozymes involved in metabolic activation of prodrugs结构和催化性能的羧酸酯酶同功酶参与代谢激活高活性化合物

Molecules 2008, 13, 412-431 molecules ISSN 1420-3049 © 2008 by MDPI /molecules Review Structure and Catalytic Properties of Carboxylesterase Isozymes Involved in Metabolic Activation of Prodrugs Masakiyo Hosokawa Laboratory of Drug Metabolism and Biopharmaceutics, Faculty of Pharmaceutical Sciences, Chiba Institute of Science, Shiomi-Cho, Choshi-City, Chiba 288-0025, Japan; E-mail: Masakiyo@cis.ac.jp Received: 14 December 2007; in revised form: 9 February 2008 / Accepted: 11 February 2008 / Published: 18 February 2008 Abstract: Mammalian carboxylesterases (CESs) comprise a multigene family whose gene products play important roles in biotransformation of ester- or amide-type prodrugs. They are members of an α,β-hydrolase-fold family and are found in various mammals. It has been suggested that CESs can be classified into five major groups denominated CES1-CES5, according to the homology of the amino acid sequence, and the majority of CESs that have been identified belong to the CES1 or CES2 family. The substrate specificities of CES1 and CES2 are significantly different. The CES1 isozyme mainly hydrolyzes a substrate with a small alcohol group and large acyl group, but its wide active pocket sometimes allows it to act on structurally distinct compounds of either a large or small alcohol moiety. In contrast, the CES2 isozyme recognizes a substrate with a large alcohol group and small acyl group, and its substrate specificity may be restricted by the capability of acyl-enzyme conjugate formation due to the presence of conformational int