2-APB inhibits volume-regulated anion channels independently from intracellular calcium signaling modulation.
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.
Lemonnier
L
L
Laboratoire de Physiologie Cellulaire, INSERM EMI 0228, Bâtiment SN3, USTL, 59655, Villeneuve d'Ascq, France.
Prevarskaya
N
N
Mazurier
J
J
Shuba
Y
Y
Skryma
R
R
D001896:Boron Compounds / Q000494:pharmacology*; D002118:Calcium / Q000378:metabolism; D020013:Calcium Signaling / Q000187:drug effects* / Q000502:physiology; D002460:Cell Line; D045744:Cell Line, Tumor; D018118:Chloride Channels / Q000037:antagonists & inhibitors*; D004305:Dose-Response Relationship, Drug; D004533:Egtazic Acid / Q000031:analogs & derivatives* / Q000494:pharmacology; D005663:Furans / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D007038:Hypotonic Solutions / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D015603:Keratinocytes / Q000187:drug effects / Q000378:metabolism; D008297:Male; D008564:Membrane Potentials / Q000187:drug effects; D018408:Patch-Clamp Techniques; D011471:Prostatic Neoplasms / Q000378:metabolism
D001896:Boron Compounds; D018118:Chloride Channels; D005663:Furans; D007038:Hypotonic Solutions; C018674:tetrahydrofuran; D004533:Egtazic Acid; C109986:2-aminoethoxydiphenyl borate; C025603:1,2-bis(2-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid; D002118:Calcium