Modulation of integrin alpha4beta1 (VLA-4) in dry eye disease

Arch Ophthalmol. 2008 Dec;126(12):1695-9. doi: 10.1001/archopht.126.12.1695.

Abstract

Objective: To study the effect of topical application of very late antigen 4 (VLA-4) small-molecule antagonist (anti-VLA-4 sm) in a mouse model of dry eye disease.

Methods: Anti-VLA-4 sm (or control vehicle) was applied topically to mice placed in a controlled-environment chamber. Corneal fluorescein staining and conjunctival T-cell enumeration were performed in the different treatment groups. Real-time polymerase chain reaction was used to quantify expression of inflammatory cytokines in the cornea and conjunctiva.

Results: Dry eye syndrome induced increased corneal fluorescein staining, corneal and conjunctival tumor necrosis factor alpha messenger RNA expression, and T-cell infiltration into the conjunctiva. Very late antigen 4 blockade significantly decreased corneal fluorescein staining compared with the untreated dry eye disease and control vehicle-treated groups (P < .001 and P = .02, respectively). In addition, VLA-4 blockade was associated with a significant decrease in conjunctival T-cell numbers (P < .001 vs control vehicle-treated group) and tumor necrosis factor-alpha transcript levels in the cornea (P = .04 vs control vehicle-treated group) and conjunctiva (P = .048 vs control vehicle-treated group).

Conclusion: Application of topical anti-VLA-4 sm led to a significant decrease in dry eye signs and suppression of inflammatory changes at the cellular and molecular levels.

Clinical relevance: Topical blockade of VLA-4 may be a novel therapeutic approach to treat the clinical signs and inflammatory changes accompanying dry eye disease.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Topical
  • Animals
  • CD3 Complex / metabolism
  • CD40 Antigens / genetics
  • Chemokine CXCL10
  • Conjunctiva / metabolism
  • Cornea / metabolism
  • Cytokines / genetics
  • Disease Models, Animal
  • Dry Eye Syndromes / genetics
  • Dry Eye Syndromes / metabolism
  • Dry Eye Syndromes / prevention & control*
  • Female
  • Fluorescein / metabolism
  • Integrin alpha4beta1 / antagonists & inhibitors*
  • Integrin alpha4beta1 / metabolism
  • Mice
  • Mice, Inbred C57BL
  • Oligopeptides / chemistry
  • Oligopeptides / pharmacology*
  • Phenylurea Compounds / chemistry
  • Phenylurea Compounds / pharmacology*
  • Polyethylene Glycols / chemistry
  • RNA, Messenger / metabolism
  • Reverse Transcriptase Polymerase Chain Reaction
  • T-Lymphocytes / physiology
  • Tumor Necrosis Factor-alpha / genetics
  • Vascular Cell Adhesion Molecule-1 / genetics

Substances

  • 2-((1-(3,5-dichlorobenzenesulfonyl)pyrrolidine-2-carbonyl)amino)-4-(4-methyl-2-(methyl-(2-(4-(3-o-tolylureido)phenyl)acetyl)amino)pentanoylamino)butyric acid
  • CD3 Complex
  • CD40 Antigens
  • Chemokine CXCL10
  • Cytokines
  • Integrin alpha4beta1
  • Oligopeptides
  • Phenylurea Compounds
  • RNA, Messenger
  • Tumor Necrosis Factor-alpha
  • Vascular Cell Adhesion Molecule-1
  • Polyethylene Glycols
  • Fluorescein