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2-Aminoethyl Diphenylborinate Analogues: Selective Inhibition for Store-Operated Ca2+ Entry

2-Aminoethyl Diphenylborinate Analogues: Selective Inhibition for Store-Operated Ca2+ Entry

Hong Zhou, Hirohide Iwasaki, Takeshi Nakamura, Kyoko Nakamura, Takayuki Maruyama, Shin-ichi Hamano, Shoichiro Ozaki, Akihiro Mizutani, Katsuhiko Mikoshiba

Biochem Biophys Res Commun. 2007 Jan 12;352(2):277-82.

PMID: 17140548

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP524958	2-Aminoethyl diphenylborinate		524-95-8	Price

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