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Triazine Thiols Decrease Apolipoprotein B Secretion From Hepatocytes Through Inhibition of Human Carboxylesterase 1.

Josef Blaszkiewicz1, Yu-Lin Jiang1, Jui-Tung Liu1

  • 1Department of Regenerative Medicine and Cell Biology, Medical University of South Carolina, Charleston, South Carolina.

Cellular and Molecular Gastroenterology and Hepatology
|April 30, 2026
PubMed
Summary
This summary is machine-generated.

Triazine thiols are novel, specific inhibitors of Carboxylesterase 1 (CES1). This discovery reveals their mechanism for reducing apolipoprotein B-100 secretion, offering a new approach for treating hypercholesterolemia.

Keywords:
ApolipoproteinCarboxylesteraseCholesterolEnzyme InhibitorHypercholesterolemiaLipoprotein MetabolismSmall Molecule

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Area of Science:

  • Biochemistry and Pharmacology
  • Genetics and Molecular Biology

Background:

  • Homozygous familial hypercholesterolemia (HoFH) is a severe genetic disorder causing high LDL cholesterol, often resistant to treatments.
  • Existing HoFH therapies have limitations, including hepatic lipid elevation and accessibility issues.
  • Triazine thiols were previously found to reduce apolipoprotein B-100 (APOB) secretion and lower cholesterol in preclinical models.

Purpose of the Study:

  • To elucidate the mechanism of action for triazine thiols in lowering cholesterol.
  • To identify the specific protein target of triazine thiols.
  • To validate CES1 inhibition as a therapeutic strategy for hypercholesterolemia.

Main Methods:

  • Affinity-based mass spectrometry to identify protein targets.
  • Biochemical assays to characterize enzyme inhibition kinetics.
  • Molecular modeling to predict binding sites.
  • CRISPR-Cas9 gene editing to create CES1-deficient cells.

Main Results:

  • Carboxylesterase 1 (CES1) was identified as the specific binding protein for triazine thiols.
  • Triazine thiols function as slow-binding, allosteric, covalent inhibitors of CES1.
  • Molecular modeling and mutation studies pinpointed Cysteine 390 as crucial for inhibition.
  • CES1-deficient cells showed reduced APOB secretion, mirroring the effect of triazine thiols.

Conclusions:

  • Triazine thiols are established as specific inhibitors of CES1.
  • CES1 inhibition is confirmed as the mechanism underlying APOB reduction by triazine thiols.
  • This research presents CES1 inhibition as a promising therapeutic avenue for managing hypercholesterolemia.