Direct modulation of volume‐regulated anion channels by Ca2+ chelating agents

FEBS Letters

Skryma, R¹  Lemonnier, L¹  Vanden Abeele, F¹  Vitko, Y²  Prevarskaya, N¹  Shuba, Y.M² 

[1] Laboratoire de Physiologie Cellulaire, INSERM EPI 9938, Bât. SN3, USTL, 59655 Villeneuve d'Ascq, France;Bogomoletz Institute of Physiology, NASU, Bogomoletz Str. 4, Kiev 01024, Ukraine

关键词: LNCaP prostate cancer cell;    Volume-regulated anion channel;    Swelling-activated chloride current;    Calcium chelating agent;    BAPTA;    EDTA;   

DOI  :  10.1016/S0014-5793(02)02863-6

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Ca²⁺ chelating agents are widely used in biological research for Ca²⁺ buffering. Here we report that BAPTA, EDTA and HEDTA produce fast, reversible, voltage-dependent inhibition of swelling-activated Cl⁻ current (I _Cl,swell) in LNCaP prostate cancer epithelial cells that is unrelated to their Ca²⁺ binding. BAPTA was the most effective (maximal blockade 67%, IC₅₀=70 μM, at +100 mV) followed by EDTA and HEDTA. I _Cl,swell blockade by EDTA was pH-dependent. BAPTA blocked I _Cl,swell also in other cell types. We conclude that Ca²⁺ chelating agents block I _Cl,swell by acting directly on the underlying channel, and that the negative charge of the free chelator form is critical for the blockade.

【 授权许可】

Unknown