alexa 2-Aminoethyl diphenylborinate analogues: selective inhibition for store-operated Ca2+ entry.
Biomedical Sciences

Biomedical Sciences

Journal of Bioengineering & Biomedical Science

Author(s): Zhou H, Iwasaki H, Nakamura T, Nakamura K, Maruyama T,

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Abstract Capacitative calcium entry (CCE), the mechanism that replenishes the internal Ca2+ stores with Ca2+ from the extracellular milieu in response to depletion of the store, is mediated by Ca2+ channels in the plasma membrane generally referred to as store-operated channels (SOCs). However, the roles of SOCs in the more physiological context have been fully elucidated. 2-Aminoethyl diphenylborinate (2-APB) strongly inhibits SOCs, as well as inositol-1,4,5 trisphosphate (IP3) receptors. In the present study, we screened a library of 166 2-APB analogues for effects on CCE and IP3-induced Ca2+ release in order to discover specific SOC inhibitors, and found that some blocked both store-operated and receptor-operated Ca2+ influx more strongly and selectively than 2-APB. Indeed, these new compounds ceased the prolonged intracellular Ca2+ oscillations induced by a low concentration of ATP in CHO-K1 cells. These novel SOC inhibitors will be valuable pharmacological and biochemical tools for elucidating the physiological roles. This article was published in Biochem Biophys Res Commun and referenced in Journal of Bioengineering & Biomedical Science

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