順天堂醫事雑誌
Online ISSN : 2188-2126
Print ISSN : 2187-9737
ISSN-L : 2187-9737
第2回学生学術奨励賞
Carboxylesterase 2: A Key Enzyme in Drug and Prodrug Metabolism
MOMOKO ISHIMINETAKEHIKO YOKOMIZOHYEON-CHEOL LEE-OKADA
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ジャーナル オープンアクセス

2020 年 66 巻 2 号 p. 120-124

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Carboxylesterases (CESs) play important roles in the metabolism of prodrugs containing ester bonds, which are often introduced to improve bioavailability and drug efficacy. CES1 and CES2 are major isozymes encoded by genes in the CES multigene family in humans, and their characteristics such as tissue distribution and substrate specificity have been extensively studied over the past few decades. This mini review briefly summarizes the current knowledge on CES2 focusing on its roles in the metabolism of anticancer prodrugs. We also discuss the regulatory mechanism of CES2 expression, which is often dysregulated in cancer cells. The development of CES2 inhibitors and methods to evaluate CES2 activity in biological samples are also discussed.

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© 2020 The Juntendo Medical Society. This is an open access article distributed under the terms of Creative Commons Attribution License (CC BY), which permits unrestricted use, distribution, and reproduction in any medium, provided the original source is properly credited.

This article is licensed under a Creative Commons [Attribution 4.0 International] license.
https://creativecommons.org/licenses/by/4.0/
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