Studies on Mustard-Stimulated Proteases and Inhibitors In Human Epidermal Keratinocytes (HEK): Development of Antivesicant Drugs

Abstract

Protease stimulation in HEK due to mustard (sulfur mustard, SM; nitrogen mustard, NM) exposure is well established. However, the specific protease(s) stimulated by mustard and the protease substrates remain to be determined. In this study, we observed that mustard stimulates several proteases, and the epidermal-dermal attachment protein laminin-5 is one of the substrates. In mustard-exposed skin, laminin-5 degradation results in the detachment of the epidermis from the dermis and, therefore, vesication. We utilized gelatin zymography, Western blotting, and immuno-fluorescence staining techniques to study the mustard-stimulated proteases and laminin-5 degradation in HEK. Two major protease bands (64 kDa and 72 kDa) were observed by zymography in mustard-exposed cells. Addition of serine protease inhibitors (50 M ICD 2812 or 1 mM PMSF), the metalloprotease inhibitor 1, 10- phenanthroline (1 mM), or the caspase inhibitor Z-VAD-FMK (10 M) to cells prior to SM exposure decreased the mustard-stimulated protease bands (zymography), and completely prevented mustardinduced laminin-5 degradation (Western blotting, immuno-fluorescence). In conclusion, our results in the HEK model indicate that (a) mustard stimulates multiple proteases in the skin, and (b) protease inhibitors are prospective vesicant countermeasures.

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Document Details

Document Type
Technical Report
Publication Date
Nov 16, 2004
Accession Number
ADA449566

Entities

People

  • Guang Xu
  • Prabhati Ray
  • Radharaman Ray
  • Xiannu Jin

Organizations

  • Walter Reed Army Institute of Research

Tags

Communities of Interest

  • Biomedical

DTIC Thesaurus Topics

  • Abstracts
  • Attachment
  • Biological Staining And Labeling
  • Chemical Warfare
  • Chemical Warfare Agents
  • Chemical Weapons
  • Degradation
  • Elements
  • Enzyme Inhibitors
  • Fluorescence
  • Inhibitors
  • Neutral Amino Acids
  • Nitrogen
  • Nitrogen Mustards
  • Skin
  • Substrates
  • Vesicants

Fields of Study

  • Biology

Readers

  • Geochemistry
  • Molecular and Cellular Biochemistry