2-APB inhibits volume-regulated anion channels independently from intracellular calcium signaling modulation

FEBS Lett. 2004 Jan 2;556(1-3):121-6. doi: 10.1016/s0014-5793(03)01387-5.

Abstract

It has previously been suggested that volume-regulated anion channels (VRACs) and store-operated channels (SOCs) interact with each other according to their expected colocalization in the plasma membrane of LNCaP cells. In order to study interactions between these two channels, we used 2-aminoethoxydiphenyl borate (2-APB) as a regular SOC inhibitor. Surprisingly 2-APB reduced VRAC activity in a dose-dependent manner (IC(50)=122.8 microM), but not 2,2-diphenyltetrahydrofuran (a structural analog of 2-APB). This effect was also present in keratinocytes. We conclude that 2-APB is an inhibitor of the VRAC family, and is also a potent tool to study the SOC-VRAC interaction in LNCaP cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Boron Compounds / pharmacology*
  • Calcium / metabolism
  • Calcium Signaling / drug effects*
  • Calcium Signaling / physiology
  • Cell Line
  • Cell Line, Tumor
  • Chloride Channels / antagonists & inhibitors*
  • Dose-Response Relationship, Drug
  • Egtazic Acid / analogs & derivatives*
  • Egtazic Acid / pharmacology
  • Furans / chemistry
  • Furans / pharmacology
  • Humans
  • Hypotonic Solutions / pharmacology
  • Inhibitory Concentration 50
  • Keratinocytes / drug effects
  • Keratinocytes / metabolism
  • Male
  • Membrane Potentials / drug effects
  • Patch-Clamp Techniques
  • Prostatic Neoplasms / metabolism

Substances

  • Boron Compounds
  • Chloride Channels
  • Furans
  • Hypotonic Solutions
  • tetrahydrofuran
  • Egtazic Acid
  • 2-aminoethoxydiphenyl borate
  • 1,2-bis(2-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid
  • Calcium