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In vitro characterization of TMPRSS2 inhibition in IPEC-J2 cells

Erzsebet Pászti-Gere1, Eszter Czimmermann1, Gabriella Ujhelyi2

  • 1a Faculty of Veterinary Science , Department of Pharmacology and Toxicology, Szent István University , Budapest , Hungary.

Journal of Enzyme Inhibition and Medicinal Chemistry
|June 10, 2016
PubMed

Insights

The synthetic TMPRSS2 inhibitor I-432 effectively suppresses trypsin-like activity in jejunal cells. This inhibition did not alter hydrogen peroxide levels, demonstrating I-432

Area of Science:

  • Biochemistry
  • Cell Biology
  • Pharmacology

Background:

  • Transmembrane serine protease, TMPRSS2, is a key target for treating influenza and implicated in prostate cancer.
  • Understanding TMPRSS2's role in cellular processes is crucial for developing targeted therapies.

Purpose of the Study:

  • To characterize the effect of the synthetic TMPRSS2 inhibitor, I-432, on jejunal IPEC-J2 cell monolayers.
  • To evaluate the efficacy of I-432 in inhibiting TMPRSS2 activity in vitro.

Main Methods:

  • Utilized IPEC-J2 cell monolayers cultured on membrane inserts.
  • Employed a fluorogenic substrate assay to measure trypsin-like activity in cell supernatants.
  • Assessed hydrogen peroxide levels and TMPRSS2 expression via immunofluorescence after I-432 treatment.

Main Results:

  • Apical administration of I-432 significantly suppressed trypsin-like activity in IPEC-J2 cell supernatants.
  • TMPRSS2 inhibition by I-432 did not affect physiological hydrogen peroxide levels.
  • Observed loss of TMPRSS2 serine protease domain expression and altered TMPRSS2 distribution post-incubation with I-432.

Conclusions:

  • The synthetic inhibitor I-432 demonstrates efficacy in suppressing TMPRSS2 activity in jejunal cells in vitro.
  • I-432 represents a potential therapeutic agent for conditions involving TMPRSS2, such as influenza and prostate cancer.
Keywords:
3-AmidinophenylalanineIPEC-J2 cellsTMPRSS2extracellular H2O2fluorogenic AMC substratetrypsin-like serine protease

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