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Human carboxylesterases: a comprehensive review.

Dandan Wang1, Liwei Zou1, Qiang Jin1

  • 1Institute of Interdisciplinary Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.

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|September 25, 2018
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Summary

Mammalian carboxylesterases (CES) are vital serine hydrolases involved in metabolizing endogenous compounds, drugs, and toxicants. Understanding CES1 and CES2 is key for developing new therapeutics and understanding their role in human health.

Keywords:
CES1CES2Human carboxylesterasesInducerInhibitor spectraSubstrate preference

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Area of Science:

  • Biochemistry
  • Pharmacology
  • Enzymology

Background:

  • Mammalian carboxylesterases (CES) are serine hydrolases crucial for metabolizing diverse substrates.
  • CES1 and CES2 are the predominant human isoforms, playing significant roles in health and xenobiotic metabolism.

Purpose of the Study:

  • To review the structural, catalytic, and functional characteristics of CES1 and CES2.
  • To summarize recent advancements in discovering CES modulators for therapeutic applications.

Main Methods:

  • Literature review of structural and catalytic features.
  • Analysis of tissue distribution, biological functions, and genetic polymorphisms.
  • Summary of substrate specificities and inhibitor properties.

Main Results:

  • CES1 and CES2 exhibit distinct properties influencing their roles in metabolism.
  • Genetic variations in CES impact their activity and substrate preference.
  • Progress in identifying CES modulators offers potential for drug development.

Conclusions:

  • CES1 and CES2 are critical targets for modulating metabolism and drug efficacy.
  • Further research into CES modulators can advance biomedical applications and drug design.