Blockade of the intermediate-conductance calcium-activated potassium channel as a new therapeutic strategy for restenosis

Circulation. 2003 Sep 2;108(9):1119-25. doi: 10.1161/01.CIR.0000086464.04719.DD. Epub 2003 Aug 25.

Abstract

Background: Angioplasty stimulates proliferation and migration of vascular smooth muscle cells (VSMC), leading to neointimal thickening and vascular restenosis. In a rat model of balloon catheter injury (BCI), we investigated whether alterations in expression of Ca2+-activated K+ channels (KCa) contribute to intimal hyperplasia and vascular restenosis.

Methods and results: Function and expression of KCa in mature medial and neointimal VSMC were characterized in situ by combined single-cell RT-PCR and patch-clamp analysis. Mature medial VSMC exclusively expressed large-conductance KCa (BKCa) channels. Two weeks after BCI, expression of BKCa was significantly reduced in neointimal VSMC, whereas expression of intermediate-conductance KCa (IKCa1) channels was upregulated. In the aortic VSMC cell line, A7r5 epidermal growth factor (EGF) induced IKCa1 upregulation and EGF-stimulated proliferation was suppressed by the selective IKCa1 blocker TRAM-34. Daily in vivo administration of TRAM-34 to rats significantly reduced intimal hyperplasia by approximately 40% at 1, 2, and 6 weeks after BCI. Two weeks of treatment with the related compound clotrimazole was equally effective. Reduction of intimal hyperplasia was accompanied by decreased neointimal cell content, with no change in the rate of apoptosis or collagen content.

Conclusions: The switch toward IKCa1 expression may promote excessive neointimal VSMC proliferation. Blockade of IKCa1 could therefore represent a new therapeutic strategy to prevent restenosis after angioplasty.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Angioplasty, Balloon / adverse effects
  • Animals
  • Cell Line
  • Cells, Cultured
  • Clotrimazole / therapeutic use
  • Epidermal Growth Factor / pharmacology
  • Graft Occlusion, Vascular / drug therapy*
  • Graft Occlusion, Vascular / etiology
  • Graft Occlusion, Vascular / pathology
  • Graft Occlusion, Vascular / physiopathology
  • Hyperplasia
  • Intermediate-Conductance Calcium-Activated Potassium Channels
  • Large-Conductance Calcium-Activated Potassium Channels
  • Muscle, Smooth, Vascular / drug effects
  • Muscle, Smooth, Vascular / metabolism
  • Muscle, Smooth, Vascular / physiopathology
  • Patch-Clamp Techniques
  • Potassium Channel Blockers / therapeutic use
  • Potassium Channels / genetics
  • Potassium Channels / metabolism*
  • Potassium Channels, Calcium-Activated / genetics
  • Potassium Channels, Calcium-Activated / metabolism
  • Pyrazoles / therapeutic use
  • RNA, Messenger / biosynthesis
  • Rats
  • Rats, Sprague-Dawley
  • Tunica Intima / cytology
  • Tunica Intima / pathology

Substances

  • Intermediate-Conductance Calcium-Activated Potassium Channels
  • Large-Conductance Calcium-Activated Potassium Channels
  • Potassium Channel Blockers
  • Potassium Channels
  • Potassium Channels, Calcium-Activated
  • Pyrazoles
  • RNA, Messenger
  • TRAM 34
  • Epidermal Growth Factor
  • Clotrimazole