Carboxylesterase 2: A Key Enzyme in Drug and Prodrug Metabolism

Abstract

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.