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Updated: Feb 1, 2026
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Highly Sensitive and Quantitative Detection of Proteins and Their Isoforms by Capillary Isoelectric Focusing Method
Published on: September 19, 2018
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Functional Study of Carboxylesterase 1 Protein Isoforms
Xinwen Wang1, Jian Shi1, Hao-Jie Zhu1
1Department of Clinical Pharmacy, University of Michigan, Ann Arbor, MI, 48109-1065, USA.
Proteomics
|December 7, 2018
Summary
Carboxylesterase 1 (CES1) protein isoforms exhibit varying activity. Isoforms 1 and 2 are major contributors to CES1 activity, influencing drug metabolism variability.
Area of Science:
- Pharmacogenomics
- Enzymology
- Drug Metabolism
Background:
- Carboxylesterase 1 (CES1) is a key human liver enzyme responsible for drug metabolism.
- Significant variability exists in individual CES1 activity and expression.
- Alternative splicing (AS) generates four CES1 protein isoforms.
Purpose of the Study:
- To investigate the activity and expression of individual CES1 isoforms.
- To determine CES1 isoform composition in human livers.
- To assess the impact of CES1 isoform composition on hepatic CES1 activity.
Main Methods:
- Utilized transfected cell lines to examine CES1 isoform expression and activity.
- Analyzed CES1 isoform composition in human liver samples.
- Correlated CES1 isoform ratios with measured CES1 activity.
Main Results:
- CES1 isoforms 3 and 4 showed reduced activity in hydrolyzing enalapril and clopidogrel compared to isoforms 1 and 2.
- Isoforms 1 and 2 constitute the majority (73-90%) of CES1 protein in human livers.
- Higher ratios of isoforms 1 and 2 to isoforms 3 and 4 correlated positively with overall CES1 activity.
Conclusions:
- CES1 isoform composition significantly impacts hepatic CES1 functional variability.
- Understanding CES1 AS regulation is crucial for optimizing pharmacotherapy involving CES1 substrates.
- Targeting CES1 isoform expression could mitigate drug response variability.
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